{"综述与进展":[{"abstractInfo":"手性芳基醇是一类重要的合成砌块，广泛存在于许多生物活性分子以及天然产物中，因此，高效高选择性地构建该类化合物是有机化学家们一直关注的研究热点.金属试剂对羰基化合物的不对称加成是构建手性芳基醇的一个简单高效的方法，其中，有机硼试剂由于其方便易得、稳定、低毒、官能团耐受性好等优点而被广泛用于醛、酮的不对称加成反应中.本文综述了过去二十年来过渡金属催化的有机硼试剂对醛、酮的不对称加成反应研究进展，并介绍了一些方法在生物活性手性分子合成中的应用.","abstractInfoCn":"手性芳基醇是一类重要的合成砌块，广泛存在于许多生物活性分子以及天然产物中，因此，高效高选择性地构建该类化合物是有机化学家们一直关注的研究热点.金属试剂对羰基化合物的不对称加成是构建手性芳基醇的一个简单高效的方法，其中，有机硼试剂由于其方便易得、稳定、低毒、官能团耐受性好等优点而被广泛用于醛、酮的不对称加成反应中.本文综述了过去二十年来过渡金属催化的有机硼试剂对醛、酮的不对称加成反应研究进展，并介绍了一些方法在生物活性手性分子合成中的应用.","abstractInfoEn":"Chiral aryl alcohols are prevalent in a broad range of biologically active compounds, pharmaceutical agents and natural products. They also constitute a broad class of optically active building blocks for the synthesis of important chiral compounds. In recent years, organoboron reagents are widely used in organic synthesis as they possess advantages of ready availability, low toxicity, good air and moisture stability as well as high functional group compatibility. Since the first report of rhodium-catalyzed asymmetric addition of aryl boronic acids to aryl aldehydes in 1998 by Miyaura, the use of organoboron reagents in asymmetric addition to various carbonyl compounds under various transition-metal catalyses has been intensively investigated. Over the past two decades, transition metal-catalyzed asymmetric addition of organoboron reagents to aldehydes and ketones has proved as one of the most direct and powerful methods for accessing versatile optically active alcohols. The development and progress of a wide range of chiral ligands for Rh, Ru, Pd, Ir, Cu, Ni and Co catalysis for asymmetric addition of organoboron reagents to aldehydes and ketones are summarized, and the achievements in enantioselective synthesis of chiral aryl alcohols and their applications in the synthesis of related biocative products are described. Among them, rhodium and ruthenium-catalyzed enantioselective additions have received considerable attention. In the cases of activated carbonyl compounds such as <i>α<\/i>-aryl ketoesters and <i>α<\/i>-diaryl diketones, excellent results can be attained in terms of both yield and enantioselectivity. However, it remains a daunting challenge for highly enantioselective addition to simple unactivated aldehydes and ketones owing to the difficulty in overcoming stereo differentiation. Future efforts in the community would focus on developing new effective transition-metal catalysts in addressing these issues by promoting efficient transformation and controlling excellent enantioselectivity.","articleNo":"","authorCnList":["祝东星"," 徐明华"],"authorEnList":["Zhu Dong-Xing"," Xu Ming-Hua"],"authorList":["祝东星"," 徐明华"],"authors":"祝东星, 徐明华","authorsCn":"祝东星, 徐明华","authorsEn":"Zhu Dong-Xing, Xu Ming-Hua","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"祝东星, 徐明华. 过渡金属催化的有机硼试剂对醛酮的不对称加成研究进展. 有机化学, 2020, 40(2): 255-275. doi: 10.6023/cjoc201910009.","citationCn":"祝东星, 徐明华. 过渡金属催化的有机硼试剂对醛酮的不对称加成研究进展. 有机化学, 2020, 40(2): 255-275. doi: 10.6023/cjoc201910009.","citationEn":"祝东星, 徐明华. Transition Metal-Catalyzed Asymmetric Addition of Organoboron Reagents to Aldehydes and Ketones. Chinese Journal of Organic Chemistry, 2020, 40(2): 255-275. doi: 10.6023/cjoc201910009.","doi":"10.6023/cjoc201910009","figContent":"yjhx-40-2-255-1.jpg$$yjhx-40-2-255-S1.jpg$$yjhx-40-2-255-S2.jpg$$yjhx-40-2-255-2.jpg$$yjhx-40-2-255-S3.jpg$$yjhx-40-2-255-S4.jpg$$yjhx-40-2-255-S5.jpg$$yjhx-40-2-255-S6.jpg$$yjhx-40-2-255-S7.jpg$$yjhx-40-2-255-S8.jpg$$yjhx-40-2-255-S9.jpg$$yjhx-40-2-255-S10.jpg$$yjhx-40-2-255-S11.jpg","figList":["yjhx-40-2-255-1.jpg","yjhx-40-2-255-S1.jpg","yjhx-40-2-255-S2.jpg","yjhx-40-2-255-2.jpg","yjhx-40-2-255-S3.jpg","yjhx-40-2-255-S4.jpg","yjhx-40-2-255-S5.jpg","yjhx-40-2-255-S6.jpg","yjhx-40-2-255-S7.jpg","yjhx-40-2-255-S8.jpg","yjhx-40-2-255-S9.jpg","yjhx-40-2-255-S10.jpg","yjhx-40-2-255-S11.jpg"],"firstFig":"yjhx-40-2-255-1.jpg","fpage":"255","highCitedState":"","htmlCount":946,"htmlFile":"","id":"457a8a41-4ecb-4ea2-be63-57e1eb4283b6","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"不对称合成, 手性醇, 有机硼试剂, 过渡金属催化, 不对称加成","keywordCn":"不对称合成, 手性醇, 有机硼试剂, 过渡金属催化, 不对称加成","keywordCnList":["不对称合成"," 手性醇"," 有机硼试剂"," 过渡金属催化"," 不对称加成"],"keywordEn":"asymmetric synthesis, chiral alcohols, organoboron reagents, transition-metal catalysis, asymmetric addition","keywordEnList":["asymmetric synthesis"," chiral alcohols"," organoboron reagents"," transition-metal catalysis"," asymmetric addition"],"keywordList":["不对称合成"," 手性醇"," 有机硼试剂"," 过渡金属催化"," 不对称加成"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"275","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":84,"pdfSize":1172.73,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"过渡金属催化的有机硼试剂对醛酮的不对称加成研究进展","titleCn":"过渡金属催化的有机硼试剂对醛酮的不对称加成研究进展","titleEn":"Transition Metal-Catalyzed Asymmetric Addition of Organoboron Reagents to Aldehydes and Ketones","viewCount":5528,"volume":"40","year":2020},{"abstractInfo":"铜（Cu）含量的高低直接影响着生命体的正常运转和自然体系的平衡.检测铜离子的方法多种多样，其中具有较高敏感度和选择性的荧光化学传感器应用更加广泛.综述了以Cu<sup>2+<\/sup>为基的荧光化学传感器通过\"替换\"法实现了对阴离子S<sup>2-<\/sup>，CN<sup>-<\/sup>，H<sub>2<\/sub>PO<sub>4<\/sub><sup>-<\/sup>，PPi和I<sup>-<\/sup>以及中性分子ATP、ADP和生物硫醇等的连续识别的研究进展.","abstractInfoCn":"铜（Cu）含量的高低直接影响着生命体的正常运转和自然体系的平衡.检测铜离子的方法多种多样，其中具有较高敏感度和选择性的荧光化学传感器应用更加广泛.综述了以Cu<sup>2+<\/sup>为基的荧光化学传感器通过\"替换\"法实现了对阴离子S<sup>2-<\/sup>，CN<sup>-<\/sup>，H<sub>2<\/sub>PO<sub>4<\/sub><sup>-<\/sup>，PPi和I<sup>-<\/sup>以及中性分子ATP、ADP和生物硫醇等的连续识别的研究进展.","abstractInfoEn":"The level of copper (Cu) directly affects the normal operation of the living body and the balance of the natural system. Fluorescence chemosensors with high sensitivity and selectivity are more widely used, although there are various methods for detecting copper ions. The research progress of fluorescence chemosensors for sequential recognition of anions S<sup>2-<\/sup>, CN<sup>-<\/sup>, H<sub>2<\/sub>PO<sub>4<\/sub><sup>-<\/sup>, PPi and I<sup>-<\/sup>, neutral molecules ATP, ADP and biological thiols by \"substitution\" method based on Cu<sup>2+<\/sup> is reviewed.","articleNo":"","authorCnList":["孟宪娇"," 赵晋忠"," 马文兵"],"authorEnList":["Meng Xianjiao"," Zhao Jinzhong"," Ma Wenbing"],"authorList":["孟宪娇"," 赵晋忠"," 马文兵"],"authors":"孟宪娇, 赵晋忠, 马文兵","authorsCn":"孟宪娇, 赵晋忠, 马文兵","authorsEn":"Meng Xianjiao, Zhao Jinzhong, Ma Wenbing","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Reviews","citation":"孟宪娇, 赵晋忠, 马文兵. 可用于连续识别Cu<sup>2+<\/sup>和阴离子、中性分子荧光探针的研究进展. 有机化学, 2020, 40(2): 276-283. doi: 10.6023/cjoc201908039.","citationCn":"孟宪娇, 赵晋忠, 马文兵. 可用于连续识别Cu<sup>2+<\/sup>和阴离子、中性分子荧光探针的研究进展. 有机化学, 2020, 40(2): 276-283. doi: 10.6023/cjoc201908039.","citationEn":"孟宪娇, 赵晋忠, 马文兵. Progress in Fluorescent Probes for Cu<sup>2+<\/sup> and Anions, Neutral Molecules Sequential Recognition. Chinese Journal of Organic Chemistry, 2020, 40(2): 276-283. doi: 10.6023/cjoc201908039.","doi":"10.6023/cjoc201908039","figContent":"","figList":[],"firstFig":"","fpage":"276","highCitedState":"","htmlCount":651,"htmlFile":"","id":"3f44c751-8e33-40a5-b38f-be6f9b327e63","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"连续识别, Cu<sup>2+<\/sup>, 荧光化学传感器, 阴离子, 生物硫醇","keywordCn":"连续识别, Cu<sup>2+<\/sup>, 荧光化学传感器, 阴离子, 生物硫醇","keywordCnList":["连续识别"," Cu<sup>2+<\/sup>"," 荧光化学传感器"," 阴离子"," 生物硫醇"],"keywordEn":"sequential recognition, Cu<sup>2+<\/sup>, fluorescence chemosensor, anion, biological thiol","keywordEnList":["sequential recognition"," Cu<sup>2+<\/sup>"," fluorescence chemosensor"," anion"," biological thiol"],"keywordList":["连续识别"," Cu<sup>2+<\/sup>"," 荧光化学传感器"," 阴离子"," 生物硫醇"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"283","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":18,"pdfSize":662.81,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"可用于连续识别Cu<sup>2+<\/sup>和阴离子、中性分子荧光探针的研究进展","titleCn":"可用于连续识别Cu<sup>2+<\/sup>和阴离子、中性分子荧光探针的研究进展","titleEn":"Progress in Fluorescent Probes for Cu<sup>2+<\/sup> and Anions, Neutral Molecules Sequential Recognition","viewCount":3647,"volume":"40","year":2020},{"abstractInfo":"硝基烯是一类重要的有机合成子，以硝基烯烃为原料，二芳基脯氨醇衍生物催化的多组分不对称串联反应是构建复杂手性化合物的重要方法，被广泛应用于有机合成和新药开发领域.根据构建的目标化合物类型，较全面地总结了基于二芳基脯氨醇衍生物催化、硝基烯为合成子的多组分不对称串联反应的合成研究，从反应的催化剂体系、反应机理、实验结果、反应优点、存在的问题和局限性等方面进行介绍，并对今后的发展做出展望.","abstractInfoCn":"硝基烯是一类重要的有机合成子，以硝基烯烃为原料，二芳基脯氨醇衍生物催化的多组分不对称串联反应是构建复杂手性化合物的重要方法，被广泛应用于有机合成和新药开发领域.根据构建的目标化合物类型，较全面地总结了基于二芳基脯氨醇衍生物催化、硝基烯为合成子的多组分不对称串联反应的合成研究，从反应的催化剂体系、反应机理、实验结果、反应优点、存在的问题和局限性等方面进行介绍，并对今后的发展做出展望.","abstractInfoEn":"Nitroolefin is an important class of organic synthons. The synthetic method of multicomponent asymmetric cascade reactions involving nitroolefin catalyzed by diarlyprolinol derivatives is quite important for the construction of complex chiral compounds. It is widely used in organic synthesis and new drugs development. In this paper, the multi-component asymmetric cascade synthesis involving nitroalkenes catalyzed by diarlyprolinol derivatives is comprehensively summarized based on the type of target compounds. In detail, the catalyst systems, reaction mechanisms, experimental results, reaction advantages, existing problems and limitations for this synthetic method are introduced respectively. The future development for this synthetic period is further evaluated as well.","articleNo":"","authorCnList":["严丽君"," 徐菡"," 王艳"," 董建伟"," 王永超"],"authorEnList":["Yan Lijun"," Xu Han"," Wang Yan"," Dong Jianwei"," Wang Yongchao"],"authorList":["严丽君"," 徐菡"," 王艳"," 董建伟"," 王永超"],"authors":"严丽君, 徐菡, 王艳, 董建伟, 王永超","authorsCn":"严丽君, 徐菡, 王艳, 董建伟, 王永超","authorsEn":"Yan Lijun, Xu Han, Wang Yan, Dong Jianwei, Wang Yongchao","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"严丽君, 徐菡, 王艳, 董建伟, 王永超. 二芳基脯氨醇衍生物催化的硝基烯参与的多组分不对称串联合成研究进展. 有机化学, 2020, 40(2): 284-299. doi: 10.6023/cjoc201909028.","citationCn":"严丽君, 徐菡, 王艳, 董建伟, 王永超. 二芳基脯氨醇衍生物催化的硝基烯参与的多组分不对称串联合成研究进展. 有机化学, 2020, 40(2): 284-299. doi: 10.6023/cjoc201909028.","citationEn":"严丽君, 徐菡, 王艳, 董建伟, 王永超. Advances in Multicomponent Asymmetric Cascade Synthesis Involving Nitroolefin Catalyzed by Diarylprolinol Derivatives. Chinese Journal of Organic Chemistry, 2020, 40(2): 284-299. doi: 10.6023/cjoc201909028.","doi":"10.6023/cjoc201909028","figContent":"yjhx-40-2-284-S1.jpg$$yjhx-40-2-284-S2.jpg$$yjhx-40-2-284-S3.jpg$$yjhx-40-2-284-S4.jpg$$yjhx-40-2-284-S5.jpg$$yjhx-40-2-284-S6.jpg$$yjhx-40-2-284-S7.jpg$$yjhx-40-2-284-S8.jpg$$yjhx-40-2-284-S9.jpg$$yjhx-40-2-284-S10.jpg$$yjhx-40-2-284-S11.jpg$$yjhx-40-2-284-S12.jpg$$yjhx-40-2-284-S13.jpg$$yjhx-40-2-284-S14.jpg$$yjhx-40-2-284-S15.jpg$$yjhx-40-2-284-S16.jpg$$yjhx-40-2-284-S17.jpg","figList":["yjhx-40-2-284-S1.jpg","yjhx-40-2-284-S2.jpg","yjhx-40-2-284-S3.jpg","yjhx-40-2-284-S4.jpg","yjhx-40-2-284-S5.jpg","yjhx-40-2-284-S6.jpg","yjhx-40-2-284-S7.jpg","yjhx-40-2-284-S8.jpg","yjhx-40-2-284-S9.jpg","yjhx-40-2-284-S10.jpg","yjhx-40-2-284-S11.jpg","yjhx-40-2-284-S12.jpg","yjhx-40-2-284-S13.jpg","yjhx-40-2-284-S14.jpg","yjhx-40-2-284-S15.jpg","yjhx-40-2-284-S16.jpg","yjhx-40-2-284-S17.jpg"],"firstFig":"yjhx-40-2-284-S1.jpg","fpage":"284","highCitedState":"","htmlCount":564,"htmlFile":"","id":"ec4e0674-df7a-42d5-9c95-9fd82e388736","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"硝基烯, 二芳基脯氨醇衍生物, 多组分反应, 不对称合成, 串联反应","keywordCn":"硝基烯, 二芳基脯氨醇衍生物, 多组分反应, 不对称合成, 串联反应","keywordCnList":["硝基烯"," 二芳基脯氨醇衍生物"," 多组分反应"," 不对称合成"," 串联反应"],"keywordEn":"nitroolefin, diarlyprolinol derivatives, multicomponent reactions, asymmetric synthesis, cascade reactions","keywordEnList":["nitroolefin"," diarlyprolinol derivatives"," multicomponent reactions"," asymmetric synthesis"," cascade reactions"],"keywordList":["硝基烯"," 二芳基脯氨醇衍生物"," 多组分反应"," 不对称合成"," 串联反应"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"299","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":12,"pdfSize":981.79,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"二芳基脯氨醇衍生物催化的硝基烯参与的多组分不对称串联合成研究进展","titleCn":"二芳基脯氨醇衍生物催化的硝基烯参与的多组分不对称串联合成研究进展","titleEn":"Advances in Multicomponent Asymmetric Cascade Synthesis Involving Nitroolefin Catalyzed by Diarylprolinol Derivatives","viewCount":3750,"volume":"40","year":2020},{"abstractInfo":"阿司匹林（ASP）是第一个合成药物，主要作为一种非甾体抗炎药而被广泛使用.具有多种生物活性，如抗血栓、抗炎和抗肿瘤等，不少文献报道了其衍生物的合成及相关活性评估.ASP现有的衍生方法分为骨架衍生、前药衍生、孪药衍生及金属配位衍生四个类别.依据修饰位点的不同，骨架衍生进一步分为C（1）-COOH位修饰、C（1）-COOH位与C（2）-OAc位同时修饰、C（2）-OAc位修饰及苯环修饰.NO-ASP是制备抗血栓衍生物的主要方法，金属配位修饰则是抗癌衍生物的主要合成方案.综述了近20年来阿司匹林的结构修饰与其活性研究进展，阐述了353种阿司匹林衍生物的合成方法及部分衍生物的药理活性，为阿司匹林衍生物的进一步开发提供参考.","abstractInfoCn":"阿司匹林（ASP）是第一个合成药物，主要作为一种非甾体抗炎药而被广泛使用.具有多种生物活性，如抗血栓、抗炎和抗肿瘤等，不少文献报道了其衍生物的合成及相关活性评估.ASP现有的衍生方法分为骨架衍生、前药衍生、孪药衍生及金属配位衍生四个类别.依据修饰位点的不同，骨架衍生进一步分为C（1）-COOH位修饰、C（1）-COOH位与C（2）-OAc位同时修饰、C（2）-OAc位修饰及苯环修饰.NO-ASP是制备抗血栓衍生物的主要方法，金属配位修饰则是抗癌衍生物的主要合成方案.综述了近20年来阿司匹林的结构修饰与其活性研究进展，阐述了353种阿司匹林衍生物的合成方法及部分衍生物的药理活性，为阿司匹林衍生物的进一步开发提供参考.","abstractInfoEn":"Aspirin (ASP), the first synthetic drug, is widely used as a non steroidal anti-inflammatory drug. It displays a variety of biological activities, such as anti-thrombosis, anti-inflammatory, anti-tumor, <i>etc<\/i>. A lot of works about the synthesis and related activity evaluation of its derivatives were reported. There are four kinds of derivatization methods:skeleton derivatization, prodrug derivatization, twin derivatization and metal coordination derivatization. According to the different modification sites, skeleton derivatization could be further divided into C(1)-COOH site modification, C(1)-COOH site and C(2)-OAc site simultaneous modification, C(2)-OAc site modification and benzene ring modification. NO-ASP is the main method to prepare antithrombotic derivatives, and metal coordination modification is the main synthesis scheme of anticancer derivatives. The structure modification and bioactivity research of aspirin in recent twenty years and the synthetic routes of 353 aspirin derivatives and the pharmacological activities of some derivatives are described, which provides a reference for the further development of aspirin derivatives.","articleNo":"","authorCnList":["张芸溪"," 高湖川"," 张程瑞"," 孙茂盛"," 陈杨杰"," 曾礼升"," 黄岚"," 陈鹏"," 黄乾明"," 蒲祥"],"authorEnList":["Zhang Yunxi"," Gao Huchuan"," Zhang Chenrui"," Sun Maosheng"," Chen Yangjie"," Zeng Lisheng"," Huang Lan"," Chen Peng"," Huang Qianming"," Pu Xiang"],"authorList":["张芸溪"," 高湖川"," 张程瑞"," 孙茂盛"," 陈杨杰"," 曾礼升"," 黄岚"," 陈鹏"," 黄乾明"," 蒲祥"],"authors":"张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥","authorsCn":"张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥","authorsEn":"Zhang Yunxi, Gao Huchuan, Zhang Chenrui, Sun Maosheng, Chen Yangjie, Zeng Lisheng, Huang Lan, Chen Peng, Huang Qianming, Pu Xiang","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Reviews","citation":"张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥. 阿司匹林的结构修饰与生物活性研究进展. 有机化学, 2020, 40(2): 300-326. doi: 10.6023/cjoc201907055.","citationCn":"张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥. 阿司匹林的结构修饰与生物活性研究进展. 有机化学, 2020, 40(2): 300-326. doi: 10.6023/cjoc201907055.","citationEn":"张芸溪, 高湖川, 张程瑞, 孙茂盛, 陈杨杰, 曾礼升, 黄岚, 陈鹏, 黄乾明, 蒲祥. Advances in the Study of Structural Modification of Aspirin and Their Biological Activities. Chinese Journal of Organic Chemistry, 2020, 40(2): 300-326. doi: 10.6023/cjoc201907055.","doi":"10.6023/cjoc201907055","figContent":"yjhx-40-2-300-S1.jpg$$yjhx-40-2-300-S2.jpg$$yjhx-40-2-300-S3.jpg$$yjhx-40-2-300-S4.jpg$$yjhx-40-2-300-S5.jpg$$yjhx-40-2-300-S6.jpg$$yjhx-40-2-300-S7.jpg$$yjhx-40-2-300-S8.jpg$$yjhx-40-2-300-S9.jpg$$yjhx-40-2-300-S10.jpg$$yjhx-40-2-300-S11.jpg$$yjhx-40-2-300-S12.jpg$$yjhx-40-2-300-S13.jpg$$yjhx-40-2-300-S14.jpg$$yjhx-40-2-300-S15.jpg$$yjhx-40-2-300-S16.jpg$$yjhx-40-2-300-S17.jpg$$yjhx-40-2-300-S18.jpg$$yjhx-40-2-300-S19.jpg$$yjhx-40-2-300-S20.jpg$$yjhx-40-2-300-S21.jpg$$yjhx-40-2-300-S22.jpg$$yjhx-40-2-300-S23.jpg$$yjhx-40-2-300-S24.jpg$$yjhx-40-2-300-S25.jpg$$yjhx-40-2-300-S26.jpg$$yjhx-40-2-300-S27.jpg$$yjhx-40-2-300-S28.jpg$$yjhx-40-2-300-S29.jpg$$yjhx-40-2-300-S30.jpg$$yjhx-40-2-300-S31.jpg$$yjhx-40-2-300-S32.jpg$$yjhx-40-2-300-S33.jpg$$yjhx-40-2-300-S34.jpg$$yjhx-40-2-300-S35.jpg$$yjhx-40-2-300-S36.jpg$$yjhx-40-2-300-S37.jpg$$yjhx-40-2-300-S38.jpg$$yjhx-40-2-300-S39.jpg$$yjhx-40-2-300-S40.jpg","figList":["yjhx-40-2-300-S1.jpg","yjhx-40-2-300-S2.jpg","yjhx-40-2-300-S3.jpg","yjhx-40-2-300-S4.jpg","yjhx-40-2-300-S5.jpg","yjhx-40-2-300-S6.jpg","yjhx-40-2-300-S7.jpg","yjhx-40-2-300-S8.jpg","yjhx-40-2-300-S9.jpg","yjhx-40-2-300-S10.jpg","yjhx-40-2-300-S11.jpg","yjhx-40-2-300-S12.jpg","yjhx-40-2-300-S13.jpg","yjhx-40-2-300-S14.jpg","yjhx-40-2-300-S15.jpg","yjhx-40-2-300-S16.jpg","yjhx-40-2-300-S17.jpg","yjhx-40-2-300-S18.jpg","yjhx-40-2-300-S19.jpg","yjhx-40-2-300-S20.jpg","yjhx-40-2-300-S21.jpg","yjhx-40-2-300-S22.jpg","yjhx-40-2-300-S23.jpg","yjhx-40-2-300-S24.jpg","yjhx-40-2-300-S25.jpg","yjhx-40-2-300-S26.jpg","yjhx-40-2-300-S27.jpg","yjhx-40-2-300-S28.jpg","yjhx-40-2-300-S29.jpg","yjhx-40-2-300-S30.jpg","yjhx-40-2-300-S31.jpg","yjhx-40-2-300-S32.jpg","yjhx-40-2-300-S33.jpg","yjhx-40-2-300-S34.jpg","yjhx-40-2-300-S35.jpg","yjhx-40-2-300-S36.jpg","yjhx-40-2-300-S37.jpg","yjhx-40-2-300-S38.jpg","yjhx-40-2-300-S39.jpg","yjhx-40-2-300-S40.jpg"],"firstFig":"yjhx-40-2-300-S1.jpg","fpage":"300","highCitedState":"","htmlCount":2523,"htmlFile":"","id":"6f58ccb8-c350-48fa-8634-4262c365dc15","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"阿司匹林, 骨架衍生, 前药衍生, 孪药衍生, 金属配位衍生","keywordCn":"阿司匹林, 骨架衍生, 前药衍生, 孪药衍生, 金属配位衍生","keywordCnList":["阿司匹林"," 骨架衍生"," 前药衍生"," 孪药衍生"," 金属配位衍生"],"keywordEn":"aspirin, skeleton derivation, prodrug derivation, twin drug derivation, metal coordination derivation","keywordEnList":["aspirin"," skeleton derivation"," prodrug derivation"," twin drug derivation"," metal coordination derivation"],"keywordList":["阿司匹林"," 骨架衍生"," 前药衍生"," 孪药衍生"," 金属配位衍生"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"326","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":109,"pdfSize":1279.48,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"阿司匹林的结构修饰与生物活性研究进展","titleCn":"阿司匹林的结构修饰与生物活性研究进展","titleEn":"Advances in the Study of Structural Modification of Aspirin and Their Biological Activities","viewCount":8968,"volume":"40","year":2020},{"abstractInfo":"3-（噁唑-5-基）吲哚类天然产物如Pimprinine，Streptochlorin等，广泛存在于海洋微生物中，因其具有多样的生物活性，在医药和农药领域中很有研究潜力.3-（噁唑-5-基）吲哚类天然产物的合成方法有很多研究报道，在吲哚结构上构建噁唑环是合成此类天然产物的关键.总结了已报道的3-（噁唑-5-基）吲哚类天然产物的生物活性，并对构建3-（噁唑-5-基）吲哚骨架的合成方法及部分主要反应机理进行了综述，探讨了3-（噁唑-5-基）吲哚类骨架作为一种优势活性结构在未来的应用前景.","abstractInfoCn":"3-（噁唑-5-基）吲哚类天然产物如Pimprinine，Streptochlorin等，广泛存在于海洋微生物中，因其具有多样的生物活性，在医药和农药领域中很有研究潜力.3-（噁唑-5-基）吲哚类天然产物的合成方法有很多研究报道，在吲哚结构上构建噁唑环是合成此类天然产物的关键.总结了已报道的3-（噁唑-5-基）吲哚类天然产物的生物活性，并对构建3-（噁唑-5-基）吲哚骨架的合成方法及部分主要反应机理进行了综述，探讨了3-（噁唑-5-基）吲哚类骨架作为一种优势活性结构在未来的应用前景.","abstractInfoEn":"3-(5-Oxazolyl)indole-type natural products such as pimprinine and streptochlorin, widely exist in marine microorganism, because of their diverse biological activity, 3-(5-oxazolyl)indoles show good research and development potential in the field of medicine and pesticide. Numerous studies have been performed to synthesize 3-(5-oxazolyl)indole-type natural products, in which the construction of indole ring and oxazole ring is the most important part. In this paper, the reported natural products with 3-(5-oxazolyl)indole skeleton structure and their biological activities are summarized, and the synthetic methods for 3-(5-oxazolyl)indole skeleton and some of their mechanism are also reviewed. The application prospect of 3-(5-oxazol-yl)indole as a dominant active structure in the future was discussed.","articleNo":"","authorCnList":["施展"," 聂克睿"," 刘畅"," 张明智"," 章维华"],"authorEnList":["Shi Zhan"," Nie Kerui"," Liu Chang"," Zhang Mingzhi"," Zhang Weihua"],"authorList":["施展"," 聂克睿"," 刘畅"," 张明智"," 章维华"],"authors":"施展, 聂克睿, 刘畅, 张明智, 章维华","authorsCn":"施展, 聂克睿, 刘畅, 张明智, 章维华","authorsEn":"Shi Zhan, Nie Kerui, Liu Chang, Zhang Mingzhi, Zhang Weihua","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"施展, 聂克睿, 刘畅, 张明智, 章维华. 3-(噁唑-5-基)吲哚类天然产物生物活性及其衍生物的合成研究进展. 有机化学, 2020, 40(2): 327-338. doi: 10.6023/cjoc201907047.","citationCn":"施展, 聂克睿, 刘畅, 张明智, 章维华. 3-(噁唑-5-基)吲哚类天然产物生物活性及其衍生物的合成研究进展. 有机化学, 2020, 40(2): 327-338. doi: 10.6023/cjoc201907047.","citationEn":"施展, 聂克睿, 刘畅, 张明智, 章维华. Biological Activities of 3-(5-Oxazolyl)indole Natural Products and Advances on Synthesis of Its Derivatives. Chinese Journal of Organic Chemistry, 2020, 40(2): 327-338. doi: 10.6023/cjoc201907047.","doi":"10.6023/cjoc201907047","figContent":"yjhx-40-2-327-S1.jpg$$yjhx-40-2-327-S2.jpg$$yjhx-40-2-327-S3.jpg$$yjhx-40-2-327-S4.jpg$$yjhx-40-2-327-S5.jpg$$yjhx-40-2-327-S6.jpg$$yjhx-40-2-327-S7.jpg$$yjhx-40-2-327-S8.jpg$$yjhx-40-2-327-S9.jpg$$yjhx-40-2-327-S10.jpg$$yjhx-40-2-327-S11.jpg$$yjhx-40-2-327-S12.jpg$$yjhx-40-2-327-S13.jpg$$yjhx-40-2-327-S14.jpg$$yjhx-40-2-327-S15.jpg$$yjhx-40-2-327-S16.jpg$$yjhx-40-2-327-S17.jpg$$yjhx-40-2-327-S18.jpg$$yjhx-40-2-327-S19.jpg$$yjhx-40-2-327-S20.jpg$$yjhx-40-2-327-S21.jpg$$yjhx-40-2-327-S22.jpg$$yjhx-40-2-327-S23.jpg$$yjhx-40-2-327-S24.jpg$$yjhx-40-2-327-S25.jpg$$yjhx-40-2-327-S26.jpg$$yjhx-40-2-327-S27.jpg$$yjhx-40-2-327-S28.jpg$$yjhx-40-2-327-S29.jpg$$yjhx-40-2-327-S30.jpg$$yjhx-40-2-327-S31.jpg$$yjhx-40-2-327-S32.jpg","figList":["yjhx-40-2-327-S1.jpg","yjhx-40-2-327-S2.jpg","yjhx-40-2-327-S3.jpg","yjhx-40-2-327-S4.jpg","yjhx-40-2-327-S5.jpg","yjhx-40-2-327-S6.jpg","yjhx-40-2-327-S7.jpg","yjhx-40-2-327-S8.jpg","yjhx-40-2-327-S9.jpg","yjhx-40-2-327-S10.jpg","yjhx-40-2-327-S11.jpg","yjhx-40-2-327-S12.jpg","yjhx-40-2-327-S13.jpg","yjhx-40-2-327-S14.jpg","yjhx-40-2-327-S15.jpg","yjhx-40-2-327-S16.jpg","yjhx-40-2-327-S17.jpg","yjhx-40-2-327-S18.jpg","yjhx-40-2-327-S19.jpg","yjhx-40-2-327-S20.jpg","yjhx-40-2-327-S21.jpg","yjhx-40-2-327-S22.jpg","yjhx-40-2-327-S23.jpg","yjhx-40-2-327-S24.jpg","yjhx-40-2-327-S25.jpg","yjhx-40-2-327-S26.jpg","yjhx-40-2-327-S27.jpg","yjhx-40-2-327-S28.jpg","yjhx-40-2-327-S29.jpg","yjhx-40-2-327-S30.jpg","yjhx-40-2-327-S31.jpg","yjhx-40-2-327-S32.jpg"],"firstFig":"yjhx-40-2-327-S1.jpg","fpage":"327","highCitedState":"","htmlCount":791,"htmlFile":"","id":"2baf8ef1-e690-493b-b0fe-6f46d8b647ba","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"3-(噁唑-5-基)吲哚, 天然产物, 生物活性, 合成, 综述","keywordCn":"3-(噁唑-5-基)吲哚, 天然产物, 生物活性, 合成, 综述","keywordCnList":["3-(噁唑-5-基)吲哚"," 天然产物"," 生物活性"," 合成"," 综述"],"keywordEn":"3-(5-oxazolyl)indole, natural products, biological activities, synthesis, review","keywordEnList":["3-(5-oxazolyl)indole"," natural products"," biological activities"," synthesis"," review"],"keywordList":["3-(噁唑-5-基)吲哚"," 天然产物"," 生物活性"," 合成"," 综述"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"338","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":51,"pdfSize":903.48,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"3-(噁唑-5-基)吲哚类天然产物生物活性及其衍生物的合成研究进展","titleCn":"3-(噁唑-5-基)吲哚类天然产物生物活性及其衍生物的合成研究进展","titleEn":"Biological Activities of 3-(5-Oxazolyl)indole Natural Products and Advances on Synthesis of Its Derivatives","viewCount":4332,"volume":"40","year":2020},{"abstractInfo":"光催化氧化还原反应具有绿色、高效、安全等优势，已经在有机化学中得到广泛关注.介绍了基于光催化的偶联/芳构化放氢反应，通过使用光催化剂/催化剂的双催化体系，可用于光催化有机碳-碳和碳-杂原子成键反应，且反应中氢气是唯一的副产物.强调了有机光氧化还原体系的构建与催化机理.","abstractInfoCn":"光催化氧化还原反应具有绿色、高效、安全等优势，已经在有机化学中得到广泛关注.介绍了基于光催化的偶联/芳构化放氢反应，通过使用光催化剂/催化剂的双催化体系，可用于光催化有机碳-碳和碳-杂原子成键反应，且反应中氢气是唯一的副产物.强调了有机光氧化还原体系的构建与催化机理.","abstractInfoEn":"The photocatalytic redox reactions have been widely concerned in organic chemistry due to their green, efficiency and safety. In this review, the cross-coupling/aromatization reactions are described based on photocatalytic organic hydrogen-evolution, which can be used to build organic carbon-carbon and carbon-heteroatom bonds by using a photocatalyst/catalyst dual catalytic system. Hydrogen is the only by-product in these reactions. The system and catalytic mechanisms of organic photocatalytic redox reaction are highlighted.","articleNo":"","authorCnList":["陈锋"," 陈浩"," 吴庆安"," 罗书平"],"authorEnList":["Chen Feng"," Chen Hao"," Wu Qing'an"," Luo Shuping"],"authorList":["陈锋"," 陈浩"," 吴庆安"," 罗书平"],"authors":"陈锋, 陈浩, 吴庆安, 罗书平","authorsCn":"陈锋, 陈浩, 吴庆安, 罗书平","authorsEn":"Chen Feng, Chen Hao, Wu Qing'an, Luo Shuping","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"陈锋, 陈浩, 吴庆安, 罗书平. 光催化有机物偶联/芳构化放氢反应研究进展. 有机化学, 2020, 40(2): 339-350. doi: 10.6023/cjoc201909024.","citationCn":"陈锋, 陈浩, 吴庆安, 罗书平. 光催化有机物偶联/芳构化放氢反应研究进展. 有机化学, 2020, 40(2): 339-350. doi: 10.6023/cjoc201909024.","citationEn":"陈锋, 陈浩, 吴庆安, 罗书平. Progress on the Photocatalytic Organic Hydrogen-Evolution Coupling/Aromatization Reaction. Chinese Journal of Organic Chemistry, 2020, 40(2): 339-350. doi: 10.6023/cjoc201909024.","doi":"10.6023/cjoc201909024","figContent":"yjhx-40-2-339-S1.jpg$$yjhx-40-2-339-S2.jpg$$yjhx-40-2-339-S3.jpg$$yjhx-40-2-339-S4.jpg$$yjhx-40-2-339-S5.jpg$$yjhx-40-2-339-S6.jpg$$yjhx-40-2-339-S7.jpg$$yjhx-40-2-339-S8.jpg$$yjhx-40-2-339-S9.jpg$$yjhx-40-2-339-S10.jpg$$yjhx-40-2-339-S11.jpg$$yjhx-40-2-339-S12.jpg$$yjhx-40-2-339-S13.jpg$$yjhx-40-2-339-S14.jpg$$yjhx-40-2-339-S15.jpg$$yjhx-40-2-339-S16.jpg$$yjhx-40-2-339-S17.jpg$$yjhx-40-2-339-S18.jpg$$yjhx-40-2-339-S19.jpg$$yjhx-40-2-339-S20.jpg$$yjhx-40-2-339-S21.jpg$$yjhx-40-2-339-S22.jpg$$yjhx-40-2-339-S23.jpg$$yjhx-40-2-339-S24.jpg$$yjhx-40-2-339-S25.jpg$$yjhx-40-2-339-S26.jpg$$yjhx-40-2-339-S27.jpg$$yjhx-40-2-339-S28.jpg","figList":["yjhx-40-2-339-S1.jpg","yjhx-40-2-339-S2.jpg","yjhx-40-2-339-S3.jpg","yjhx-40-2-339-S4.jpg","yjhx-40-2-339-S5.jpg","yjhx-40-2-339-S6.jpg","yjhx-40-2-339-S7.jpg","yjhx-40-2-339-S8.jpg","yjhx-40-2-339-S9.jpg","yjhx-40-2-339-S10.jpg","yjhx-40-2-339-S11.jpg","yjhx-40-2-339-S12.jpg","yjhx-40-2-339-S13.jpg","yjhx-40-2-339-S14.jpg","yjhx-40-2-339-S15.jpg","yjhx-40-2-339-S16.jpg","yjhx-40-2-339-S17.jpg","yjhx-40-2-339-S18.jpg","yjhx-40-2-339-S19.jpg","yjhx-40-2-339-S20.jpg","yjhx-40-2-339-S21.jpg","yjhx-40-2-339-S22.jpg","yjhx-40-2-339-S23.jpg","yjhx-40-2-339-S24.jpg","yjhx-40-2-339-S25.jpg","yjhx-40-2-339-S26.jpg","yjhx-40-2-339-S27.jpg","yjhx-40-2-339-S28.jpg"],"firstFig":"yjhx-40-2-339-S1.jpg","fpage":"339","highCitedState":"","htmlCount":910,"htmlFile":"","id":"79708b9b-b500-4741-abae-3823c05cf38b","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"光催化, 有机物放氢反应, 偶联反应, 芳构化反应","keywordCn":"光催化, 有机物放氢反应, 偶联反应, 芳构化反应","keywordCnList":["光催化"," 有机物放氢反应"," 偶联反应"," 芳构化反应"],"keywordEn":"photocatalysis, organic hydrogen-evolution reaction, coupling reaction, aromatization reaction","keywordEnList":["photocatalysis"," organic hydrogen-evolution reaction"," coupling reaction"," aromatization reaction"],"keywordList":["光催化"," 有机物放氢反应"," 偶联反应"," 芳构化反应"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"350","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":84,"pdfSize":991.41,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"光催化有机物偶联/芳构化放氢反应研究进展","titleCn":"光催化有机物偶联/芳构化放氢反应研究进展","titleEn":"Progress on the Photocatalytic Organic Hydrogen-Evolution Coupling/Aromatization Reaction","viewCount":4750,"volume":"40","year":2020},{"abstractInfo":"醌式杂环（噻吩、吡咯、呋喃等）分子具有结构刚性、最高占据分子轨道（HOMO）/最低未占据分子轨道（LUMO）能级低、能级带隙窄和摩尔消光系数高等特点.醌式分子因其结构平面性特点，分子间作用力较强，因而分子间电荷传输能力强.目前，醌式杂环分子已成为有机半导体材料领域特别是有机场效应晶体管领域的研究热点.根据醌式杂环分子的结构特点，以端基为分类依据，综述了近年来醌式杂环化合物在分子设计、合成及应用性能等方面的研究进展，并展望了醌式杂环分子的发展前景.","abstractInfoCn":"醌式杂环（噻吩、吡咯、呋喃等）分子具有结构刚性、最高占据分子轨道（HOMO）/最低未占据分子轨道（LUMO）能级低、能级带隙窄和摩尔消光系数高等特点.醌式分子因其结构平面性特点，分子间作用力较强，因而分子间电荷传输能力强.目前，醌式杂环分子已成为有机半导体材料领域特别是有机场效应晶体管领域的研究热点.根据醌式杂环分子的结构特点，以端基为分类依据，综述了近年来醌式杂环化合物在分子设计、合成及应用性能等方面的研究进展，并展望了醌式杂环分子的发展前景.","abstractInfoEn":"Quinoidal heterocyclic (thiophene, pyrrole, furan, <i>etc<\/i>.) molecules have the characteristics of rigid backbone, low highest occupied molecular orbital (HOMO)/lowest unoccupied molecular orbital (LUMO) level, narrow band gap and high molar extinction coefficient, and so on. Because of their planar structures, quinoidal molecules usually have strong intermolecular charge transfer ability due to the strong intermolecular interaction. Up to now, quinoidal heterocyclic molecules have become a research hotspot in the field of organic semiconductor materials, especially in the field of organic field effect transistors. According to the structural features of quinoidal heterocyclic molecules and the classification basis of terminal groups, the research progress of quinoidal heterocyclic compounds in molecular design, synthesis and application in recent years is reviewed, and the development of quinoidal heterocyclic molecules is prospected.","articleNo":"","authorCnList":["蔡金芳"," 江华"," 崔志华"," 陈维国"],"authorEnList":["Cai Jinfang"," Jiang Hua"," Cui Zhihua"," Chen Weiguo"],"authorList":["蔡金芳"," 江华"," 崔志华"," 陈维国"],"authors":"蔡金芳, 江华, 崔志华, 陈维国","authorsCn":"蔡金芳, 江华, 崔志华, 陈维国","authorsEn":"Cai Jinfang, Jiang Hua, Cui Zhihua, Chen Weiguo","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"蔡金芳, 江华, 崔志华, 陈维国. 醌式杂环化合物的设计、合成及应用性能研究进展. 有机化学, 2020, 40(2): 351-363. doi: 10.6023/cjoc201909022.","citationCn":"蔡金芳, 江华, 崔志华, 陈维国. 醌式杂环化合物的设计、合成及应用性能研究进展. 有机化学, 2020, 40(2): 351-363. doi: 10.6023/cjoc201909022.","citationEn":"蔡金芳, 江华, 崔志华, 陈维国. Research Progress in Design, Synthesis and Application for Quinoidal Heterocyclic Compounds. Chinese Journal of Organic Chemistry, 2020, 40(2): 351-363. doi: 10.6023/cjoc201909022.","doi":"10.6023/cjoc201909022","figContent":"yjhx-40-2-351-S1.jpg$$yjhx-40-2-351-S2.jpg$$yjhx-40-2-351-S3.jpg$$yjhx-40-2-351-S4.jpg$$yjhx-40-2-351-S5.jpg$$yjhx-40-2-351-S6.jpg$$yjhx-40-2-351-S7.jpg$$yjhx-40-2-351-S8.jpg$$yjhx-40-2-351-S9.jpg$$yjhx-40-2-351-S10.jpg$$yjhx-40-2-351-S11.jpg","figList":["yjhx-40-2-351-S1.jpg","yjhx-40-2-351-S2.jpg","yjhx-40-2-351-S3.jpg","yjhx-40-2-351-S4.jpg","yjhx-40-2-351-S5.jpg","yjhx-40-2-351-S6.jpg","yjhx-40-2-351-S7.jpg","yjhx-40-2-351-S8.jpg","yjhx-40-2-351-S9.jpg","yjhx-40-2-351-S10.jpg","yjhx-40-2-351-S11.jpg"],"firstFig":"yjhx-40-2-351-S1.jpg","fpage":"351","highCitedState":"","htmlCount":1604,"htmlFile":"","id":"eb796334-a4d9-4ed2-8846-69a80cf4fecc","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"醌式杂环化合物, 设计与合成, 性质与应用, 有机半导体材料, 有机场效应晶体管","keywordCn":"醌式杂环化合物, 设计与合成, 性质与应用, 有机半导体材料, 有机场效应晶体管","keywordCnList":["醌式杂环化合物"," 设计与合成"," 性质与应用"," 有机半导体材料"," 有机场效应晶体管"],"keywordEn":"quinoidal heterocyclic compound, design and synthesis, property and application, organic semiconductor material, organic field effect transistors","keywordEnList":["quinoidal heterocyclic compound"," design and synthesis"," property and application"," organic semiconductor material"," organic field effect transistors"],"keywordList":["醌式杂环化合物"," 设计与合成"," 性质与应用"," 有机半导体材料"," 有机场效应晶体管"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"363","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":113,"pdfSize":757.38,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"醌式杂环化合物的设计、合成及应用性能研究进展","titleCn":"醌式杂环化合物的设计、合成及应用性能研究进展","titleEn":"Research Progress in Design, Synthesis and Application for Quinoidal Heterocyclic Compounds","viewCount":5891,"volume":"40","year":2020},{"abstractInfo":"由于离散型金属环状化合物在主客体化学、气体吸附、分子识别及催化等领域被广泛应用，因此，构筑新型金属环状化合物并研究它们的物理化学性质及应用成为无机化学、有机化学和超分子化学中热门研究方向之一.具有半夹心结构的钌、铱和铑有机金属单元在形成金属环状化合物时具有以下的优势：增强了化合物的溶解性，屏蔽住金属的一半以减少反应的复杂性，易于修饰得到不同结构的产物.综述了近年来以半夹心结构的钌、铱和铑结构基元的离散型金属框架化合物的组装合成和应用.","abstractInfoCn":"由于离散型金属环状化合物在主客体化学、气体吸附、分子识别及催化等领域被广泛应用，因此，构筑新型金属环状化合物并研究它们的物理化学性质及应用成为无机化学、有机化学和超分子化学中热门研究方向之一.具有半夹心结构的钌、铱和铑有机金属单元在形成金属环状化合物时具有以下的优势：增强了化合物的溶解性，屏蔽住金属的一半以减少反应的复杂性，易于修饰得到不同结构的产物.综述了近年来以半夹心结构的钌、铱和铑结构基元的离散型金属框架化合物的组装合成和应用.","abstractInfoEn":"Discrete metallacycle complexes have attracted considerable attention because of their widely used in host-guest chemistry, gas adsorption, molecular recognition and catalysis. Thus exploring new framework complexes, studying their physical and chemical properties and applications have become one of the most active and exciting areas of inorganic chemistry, organic chemistry and supramolecular chemistry. Half-sandwich organometallic units based on ruthenium, iridium and rhodium are often utilized to prepare diverse metallacylce complexes due to the following advantages:the solubility of these metal complexes can be enhanced, the hemisphere of the metal center is perfectly shielded, minimizing the complexity of reactions, and the products with different structures are easily synthesized. In this paper, the synthesis and application of discrete type metal framework complexes with half-sandwich structures of ruthenium, iridium and rhodium are reviewed.","articleNo":"","authorCnList":["刘金宝"," 李鹏"," 姚子健"],"authorEnList":["Liu Jinbao"," Li Peng"," Yao Zijian"],"authorList":["刘金宝"," 李鹏"," 姚子健"],"authors":"刘金宝, 李鹏, 姚子健","authorsCn":"刘金宝, 李鹏, 姚子健","authorsEn":"Liu Jinbao, Li Peng, Yao Zijian","categoryName":"综述与进展","categoryNameCn":"综述与进展","categoryNameEn":"Review","citation":"刘金宝, 李鹏, 姚子健. 含半夹心铱/铑/钌结构基元的离散型金属环状化合物的研究进展. 有机化学, 2020, 40(2): 364-375. doi: 10.6023/cjoc201908009.","citationCn":"刘金宝, 李鹏, 姚子健. 含半夹心铱/铑/钌结构基元的离散型金属环状化合物的研究进展. 有机化学, 2020, 40(2): 364-375. doi: 10.6023/cjoc201908009.","citationEn":"刘金宝, 李鹏, 姚子健. Recent Progress of Discrete Metallacycles Based on the Half-Sandwich Ir/Rh/Ru Motifs. Chinese Journal of Organic Chemistry, 2020, 40(2): 364-375. doi: 10.6023/cjoc201908009.","doi":"10.6023/cjoc201908009","figContent":"yjhx-40-2-364-1.jpg$$yjhx-40-2-364-2.jpg$$yjhx-40-2-364-3.jpg$$yjhx-40-2-364-4.jpg$$yjhx-40-2-364-5.jpg$$yjhx-40-2-364-6.jpg$$yjhx-40-2-364-7.jpg$$yjhx-40-2-364-8.jpg$$yjhx-40-2-364-9.jpg$$yjhx-40-2-364-10.jpg$$yjhx-40-2-364-11.jpg$$yjhx-40-2-364-12.jpg$$yjhx-40-2-364-13.jpg$$yjhx-40-2-364-14.jpg$$yjhx-40-2-364-15.jpg$$yjhx-40-2-364-16.jpg$$yjhx-40-2-364-17.jpg$$yjhx-40-2-364-18.jpg$$yjhx-40-2-364-19.jpg$$yjhx-40-2-364-20.jpg","figList":["yjhx-40-2-364-1.jpg","yjhx-40-2-364-2.jpg","yjhx-40-2-364-3.jpg","yjhx-40-2-364-4.jpg","yjhx-40-2-364-5.jpg","yjhx-40-2-364-6.jpg","yjhx-40-2-364-7.jpg","yjhx-40-2-364-8.jpg","yjhx-40-2-364-9.jpg","yjhx-40-2-364-10.jpg","yjhx-40-2-364-11.jpg","yjhx-40-2-364-12.jpg","yjhx-40-2-364-13.jpg","yjhx-40-2-364-14.jpg","yjhx-40-2-364-15.jpg","yjhx-40-2-364-16.jpg","yjhx-40-2-364-17.jpg","yjhx-40-2-364-18.jpg","yjhx-40-2-364-19.jpg","yjhx-40-2-364-20.jpg"],"firstFig":"yjhx-40-2-364-1.jpg","fpage":"364","highCitedState":"","htmlCount":867,"htmlFile":"","id":"fe6bf91f-7a96-4922-91c7-abb2dbfef76b","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"有机金属, 半夹心, 铱/铑/钌, 金属大环","keywordCn":"有机金属, 半夹心, 铱/铑/钌, 金属大环","keywordCnList":["有机金属"," 半夹心"," 铱/铑/钌"," 金属大环"],"keywordEn":"organometallic, half-sandwich, Ir/Rh/Ru, metallacycle","keywordEnList":["organometallic"," half-sandwich"," Ir/Rh/Ru"," metallacycle"],"keywordList":["有机金属"," 半夹心"," 铱/铑/钌"," 金属大环"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"375","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":21,"pdfSize":5077.36,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"含半夹心铱/铑/钌结构基元的离散型金属环状化合物的研究进展","titleCn":"含半夹心铱/铑/钌结构基元的离散型金属环状化合物的研究进展","titleEn":"Recent Progress of Discrete Metallacycles Based on the Half-Sandwich Ir/Rh/Ru Motifs","viewCount":4297,"volume":"40","year":2020}],"Articles":[{"abstractInfo":"<i>N<\/i><sup>3<\/sup>-Purinenucleosidecanbeemployedasapotentdualinhibitortoinhibitvirusesmoreeffectivelybecauseitcouldbepossiblyrecognizedbybothpurine-andpyrimidine-metabolizingenzymes.Herein,anasymmetrictransferhydrogenationviadynamickineticresolutionof<i>rac<\/i>-<i>α<\/i>-(purin-3-yl)cyclopentoneshasbeendevelopedtoproduceawiderangeofcarbocyclic<i>N<\/i><sup>3<\/sup>-purinenucleosidesinhighyieldsandexcellentstereoselectivities.Moreover,thecatalyticsystemwassuitablefor<i>rac<\/i>-<i>α<\/i>-pyrimidinylcyclopentones.Withadditionaltransformations,several2'-F-,AcS-,N<sub>3<\/sub>-modifiedcarbocyclicnucleosidescouldbeobtainedwithgoodtoexcellentyieldsandexcellentenantioselectivities.","abstractInfoCn":"<i>N<\/i><sup>3<\/sup>-嘌呤核苷由于可能同时被嘌呤和嘧啶代谢酶识别，因而有望作为双靶点药物应用于抗病毒治疗.报道了一种以<i>α<\/i>-（<i>N<\/i><sup>3<\/sup>-嘌呤）取代的环烷酮为原料，通过不对称氢转移反应实现动态动力学拆分，高收率高立体选择性地合成系列碳环<i>N<\/i><sup>3<\/sup>-嘌呤核苷化合物.该催化体系也适用于<i>α<\/i>-嘧啶取代的环烷酮底物，且产物通过进一步衍生，合成了2'-F-，AcS-，N<sub>3<\/sub>-修饰的碳环嘧啶核苷.","abstractInfoEn":"<i>N<\/i><sup>3<\/sup>-Purine nucleoside can be employed as a potent dual inhibitor to inhibit viruses more effectively because it could be possibly recognized by both purine-and pyrimidine-metabolizing enzymes. Herein, an asymmetric transfer hydrogenation via dynamic kinetic resolution of <i>rac<\/i>-<i>α<\/i>-(purin-3-yl)cyclopentones has been developed to produce a wide range of carbocyclic <i>N<\/i><sup>3<\/sup>-purine nucleosides in high yields and excellent stereoselectivities. Moreover, the catalytic system was suitable for <i>rac<\/i>-<i>α<\/i>-pyrimidinyl cyclopentones. With additional transformations, several 2'-F-, AcS-, N<sub>3<\/sub>-modified carbocyclic nucleosides could be obtained with good to excellent yields and excellent enantioselectivities.","articleNo":"","authorCnList":["张齐英"," 张一铭"," 郝二军"," 白娟"," 渠桂荣"," 郭海明"],"authorEnList":["Zhang Qiying"," Zhang Yiming"," Hao Erjun"," Bai Juan"," Qu Guirong"," Guo Haiming"],"authorList":["Zhang Qiying"," Zhang Yiming"," Hao Erjun"," Bai Juan"," Qu Guirong"," Guo Haiming"],"authors":"Zhang Qiying, Zhang Yiming, Hao Erjun, Bai Juan, Qu Guirong, Guo Haiming","authorsCn":"张齐英, 张一铭, 郝二军, 白娟, 渠桂荣, 郭海明","authorsEn":"Zhang Qiying, Zhang Yiming, Hao Erjun, Bai Juan, Qu Guirong, Guo Haiming","categoryName":"Articles","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"Zhang Qiying, Zhang Yiming, Hao Erjun, Bai Juan, Qu Guirong, Guo Haiming. Asymmetric Transfer Hydrogenation via Dynamic Kinetic Resolution for the Construction of Carbocyclic <i>N<\/i><sup>3<\/sup>-Purine Nucleosides. Chinese Journal of Organic Chemistry, 2020, 40(2): 376-383. doi: 10.6023/cjoc201907053.","citationCn":"Zhang Qiying, Zhang Yiming, Hao Erjun, Bai Juan, Qu Guirong, Guo Haiming. 通过不对称氢转移/动态动力学拆分合成碳环<i>N<\/i><sup>3<\/sup>-嘌呤核苷. 有机化学, 2020, 40(2): 376-383. doi: 10.6023/cjoc201907053.","citationEn":"Zhang Qiying, Zhang Yiming, Hao Erjun, Bai Juan, Qu Guirong, Guo Haiming. Asymmetric Transfer Hydrogenation via Dynamic Kinetic Resolution for the Construction of Carbocyclic <i>N<\/i><sup>3<\/sup>-Purine Nucleosides. Chinese Journal of Organic Chemistry, 2020, 40(2): 376-383. doi: 10.6023/cjoc201907053.","doi":"10.6023/cjoc201907053","figContent":"yjhx-40-2-376-1.jpg$$yjhx-40-2-376-S1.jpg$$yjhx-40-2-376-S2.jpg$$yjhx-40-2-376-S3.jpg","figList":["yjhx-40-2-376-1.jpg","yjhx-40-2-376-S1.jpg","yjhx-40-2-376-S2.jpg","yjhx-40-2-376-S3.jpg"],"firstFig":"yjhx-40-2-376-1.jpg","fpage":"376","highCitedState":"","htmlCount":211,"htmlFile":"","id":"b3152a7c-26ab-4868-8768-3d6083864805","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"carbocyclic nucleosides, dual inhibitors, dynamic kinetic resolution, asymmetric transfer hydrogenation","keywordCn":"碳环核苷, 双靶点抑制剂, 动态动力学拆分, 不对称氢转移反应","keywordCnList":["碳环核苷"," 双靶点抑制剂"," 动态动力学拆分"," 不对称氢转移反应"],"keywordEn":"carbocyclic nucleosides, dual inhibitors, dynamic kinetic resolution, asymmetric transfer hydrogenation","keywordEnList":["carbocyclic nucleosides"," dual inhibitors"," dynamic kinetic resolution"," asymmetric transfer hydrogenation"],"keywordList":["carbocyclic nucleosides"," dual inhibitors"," dynamic kinetic resolution"," asymmetric transfer hydrogenation"],"language":"en","latestInfo":"","latestState":"","latestStateEn":"","lpage":"383","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":14,"pdfSize":629.27,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"Asymmetric Transfer Hydrogenation via Dynamic Kinetic Resolution for the Construction of Carbocyclic <i>N<\/i><sup>3<\/sup>-Purine Nucleosides","titleCn":"通过不对称氢转移/动态动力学拆分合成碳环<i>N<\/i><sup>3<\/sup>-嘌呤核苷","titleEn":"Asymmetric Transfer Hydrogenation via Dynamic Kinetic Resolution for the Construction of Carbocyclic <i>N<\/i><sup>3<\/sup>-Purine Nucleosides","viewCount":1968,"volume":"40","year":2020},{"abstractInfo":"Inordertofindhigh-efficiencyantitumordrugs,aseriesof2,4,6-trisubstitutedpyrimidinederivativescontainingbenzothiazolemoietyweredesigned,synthesizedandevaluatedforantitumoractivitiesagainstfourcancercells(EC-109,humanesophagealcancercells;MGC-803,humangastriccancercells;PC-3,humanprostatecancercells;HepG-2,humanlivercancercells),GES-1(humannormalgastricmucosalepithelialcells),andHEEC(humannormalesophagus)usingthiazolylblue(MTT)method.TheresultsshowedthatsomecompoundsexhibitedmoderatetostrongantitumoractivitiesagainstMGC-803andPC-3cells.Amongthem,2-(((4-(4-(pyridin-2-yl)piperazin-1-yl)-6-(trifluoromethyl)pyrimidin-2-yl)-thio)methyl)benzo[d]thiazole(<b>13h<\/b>)and2-(((4-(4-(pyrimidin-2-yl)piperazin-1-yl)-6-(trifluoromethyl)pyrimidin-2-yl)thio)-methyl)benzo[<i>d<\/i>]thiazole(<b>13i<\/b>)showedthemostpotentantitumoractivitiesagainstPC-3cellswithIC<sub>50<\/sub>valuesof3.82and2.29μmol/L,respectively.Thetoxicitiesofcompounds<b>13h<\/b>and<b>13i<\/b>toGES-1cellsweresignificantlylowerthanthepositivecontrol5-fluorouracil.","abstractInfoCn":"为了寻找高效的抗肿瘤药物，设计并合成了一系列含苯并噻唑砌块的2，4，6-三取代嘧啶衍生物.采用噻唑蓝（MTT）法对目标化合物在人类四种癌细胞[EC-109（人食管癌细胞）、MGC-803（人胃癌细胞）、PC-3（人前列腺癌细胞）、HepG-2（人肝癌细胞）]、GES-1（人正常胃黏膜上皮细胞）和HEEC（人正常食管细胞）中进行抗肿瘤活性评价，结果显示部分化合物对MGC-803和PC-3细胞表现出中度至强效的抗肿瘤活性.其中2-（（（4-（4-（吡啶-2-基）哌嗪-1-基）-6-（三氟甲基）嘧啶-2-基）硫基）甲基）苯并[<i>d<\/i>]噻唑（<b>13h<\/b>）和2-（（（4-（4-（嘧啶-2-基）哌嗪-1-基）-6-（三-氟甲基）嘧啶-2-基）硫代）甲基）苯并[<i>d<\/i>]噻唑（<b>13i<\/b>）对PC-3表现出比较好的抗肿瘤活性，IC<sub>50<\/sub>值分别3.82和2.29μmol/L，且化合物<b>13h<\/b>和<b>13i<\/b>对GES-1的细胞增值毒性明显小于阳性对照5-氟尿嘧啶.","abstractInfoEn":"In order to find high-efficiency antitumor drugs, a series of 2, 4, 6-trisubstituted pyrimidine derivatives containing benzothiazole moiety were designed, synthesized and evaluated for antitumor activities against four cancer cells (EC-109, human esophageal cancer cells; MGC-803, human gastric cancer cells; PC-3, human prostate cancer cells; HepG-2, human liver cancer cells), GES-1 (human normal gastric mucosal epithelial cells), and HEEC (human normal esophagus) using thiazolyl blue (MTT) method. The results showed that some compounds exhibited moderate to strong antitumor activities against MGC-803 and PC-3 cells. Among them, 2-(((4-(4-(pyridin-2-yl)piperazin-1-yl)-6-(trifluoromethyl)pyrimidin-2-yl)-thio)methyl)benzo[d]thiazole (<b>13h<\/b>) and 2-(((4-(4-(pyrimidin-2-yl)piperazin-1-yl)-6-(trifluoromethyl)pyrimidin-2-yl)thio)-methyl)benzo[<i>d<\/i>]thiazole (<b>13i<\/b>) showed the most potent antitumor activities against PC-3 cells with IC<sub>50<\/sub> values of 3.82 and 2.29 μmol/L, respectively. The toxicities of compounds <b>13h<\/b> and <b>13i<\/b> to GES-1 cells were significantly lower than the positive control 5-fluorouracil.","articleNo":"","authorCnList":["李二冬"," 孟娅琪"," 张路野"," 张洋"," 周蕊"," 刘丽敏"," 栗娜"," 辛景超"," 郑甲信"," 单丽红"," 刘宏民"," 张秋荣"],"authorEnList":["Li Erdong"," Meng Yaqi"," Zhang Luye"," Zhang Yang"," Zhou Rui"," Liu Limin"," Li Nab"," Xin Jingchao"," Zheng Jiaxin"," Shan Lihong"," Liu Hongmin"," Zhang Qiurong"],"authorList":["Li Erdong"," Meng Yaqi"," Zhang Luye"," Zhang Yang"," Zhou Rui"," Liu Limin"," Li Nab"," Xin Jingchao"," Zheng Jiaxin"," Shan Lihong"," Liu Hongmin"," Zhang Qiurong"],"authors":"Li Erdong, Meng Yaqi, Zhang Luye, Zhang Yang, Zhou Rui, Liu Limin, Li Nab, Xin Jingchao, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong","authorsCn":"李二冬, 孟娅琪, 张路野, 张洋, 周蕊, 刘丽敏, 栗娜, 辛景超, 郑甲信, 单丽红, 刘宏民, 张秋荣","authorsEn":"Li Erdong, Meng Yaqi, Zhang Luye, Zhang Yang, Zhou Rui, Liu Limin, Li Nab, Xin Jingchao, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong","categoryName":"Articles","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"Li Erdong, Meng Yaqi, Zhang Luye, Zhang Yang, Zhou Rui, Liu Limin, Li Nab, Xin Jingchao, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives Containing Benzothiazole Moiety. Chinese Journal of Organic Chemistry, 2020, 40(2): 417-422. doi: 10.6023/cjoc201907016.","citationCn":"Li Erdong, Meng Yaqi, Zhang Luye, Zhang Yang, Zhou Rui, Liu Limin, Li Nab, Xin Jingchao, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong. 含苯并噻唑砌块的2, 4, 6-三取代嘧啶衍生物的合成及抗肿瘤活性评价. 有机化学, 2020, 40(2): 417-422. doi: 10.6023/cjoc201907016.","citationEn":"Li Erdong, Meng Yaqi, Zhang Luye, Zhang Yang, Zhou Rui, Liu Limin, Li Nab, Xin Jingchao, Zheng Jiaxin, Shan Lihong, Liu Hongmin, Zhang Qiurong. Synthesis and Antitumor Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives Containing Benzothiazole Moiety. Chinese Journal of Organic Chemistry, 2020, 40(2): 417-422. doi: 10.6023/cjoc201907016.","doi":"10.6023/cjoc201907016","figContent":"yjhx-40-2-417-1.jpg$$yjhx-40-2-417-S1.jpg","figList":["yjhx-40-2-417-1.jpg","yjhx-40-2-417-S1.jpg"],"firstFig":"yjhx-40-2-417-1.jpg","fpage":"417","highCitedState":"","htmlCount":261,"htmlFile":"","id":"06f1c442-d5ff-4357-80dc-8f8a88a6cd73","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"pyrimidine, benzothiazole, synthesis, antitumor activity","keywordCn":"嘧啶, 苯并噻唑, 合成, 抗肿瘤活性","keywordCnList":["嘧啶"," 苯并噻唑"," 合成"," 抗肿瘤活性"],"keywordEn":"pyrimidine, benzothiazole, synthesis, antitumor activity","keywordEnList":["pyrimidine"," benzothiazole"," synthesis"," antitumor activity"],"keywordList":["pyrimidine"," benzothiazole"," synthesis"," antitumor activity"],"language":"en","latestInfo":"","latestState":"","latestStateEn":"","lpage":"422","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":12,"pdfSize":460.96,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"Synthesis and Antitumor Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives Containing Benzothiazole Moiety","titleCn":"含苯并噻唑砌块的2, 4, 6-三取代嘧啶衍生物的合成及抗肿瘤活性评价","titleEn":"Synthesis and Antitumor Evaluation of 2, 4, 6-Trisubstituted Pyrimidine Derivatives Containing Benzothiazole Moiety","viewCount":2374,"volume":"40","year":2020},{"abstractInfo":"Asilver-mediatedalkynylphosphonationof1,4-enyneswithdiarylphosphineoxideshasbeendeveloped,bywhichawiderangeof<i>γ<\/i>-ketophosphineoxideswithmoderatetogoodyieldsweresynthesizedthroughradical1,2-alkynylmigration.ThetransformationproceededwithsequentialP-centeredradicaladditiontovinylunit,3-<i>exo-dig<\/i>cyclizationand1,2-alkynylmigration,resultinginthebond-formingeventsincludingC-PandC-Cbondstorealizedifunctionalizationofunactivatedolefins.","abstractInfoCn":"研究了1，4-烯炔衍生物与二芳基膦氧化物在银介导下发生的炔酰化反应.该反应利用自由基引发的1，2-炔基迁移策略合成了一系列<i>γ<\/i>-酮膦氧化物，产率适中.该反应机理可能涉及膦中心自由基与乙烯基的加成、3-<i>exo-dig<\/i>环化和1，2-炔基迁移等连续的过程，一步形成了C-P、C-C键等化学键，实现了非活性烯烃的双官能化.","abstractInfoEn":"A silver-mediated alkynylphosphonation of 1, 4-enynes with diarylphosphine oxides has been developed, by which a wide range of <i>γ<\/i>-ketophosphine oxides with moderate to good yields were synthesized through radical 1, 2-alkynyl migration. The transformation proceeded with sequential P-centered radical addition to vinyl unit, 3-<i>exo-dig<\/i> cyclization and 1, 2-alkynyl migration, resulting in the bond-forming events including C-P and C-C bonds to realize difunctionalization of unactivated olefins.","articleNo":"","authorCnList":["张萍"," 石浩楠"," 张天舒"," 蔡佩君"," 姜波"," 屠树江"],"authorEnList":["Zhang Ping"," Shi Haonan"," Zhang Tianshu"," Cai Peijun"," Jiang Bo"," Tu Shujiang"],"authorList":["Zhang Ping"," Shi Haonan"," Zhang Tianshu"," Cai Peijun"," Jiang Bo"," Tu Shujiang"],"authors":"Zhang Ping, Shi Haonan, Zhang Tianshu, Cai Peijun, Jiang Bo, Tu Shujiang","authorsCn":"张萍, 石浩楠, 张天舒, 蔡佩君, 姜波, 屠树江","authorsEn":"Zhang Ping, Shi Haonan, Zhang Tianshu, Cai Peijun, Jiang Bo, Tu Shujiang","categoryName":"Articles","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"Zhang Ping, Shi Haonan, Zhang Tianshu, Cai Peijun, Jiang Bo, Tu Shujiang. Alkynylphosphonation of Unactivated Olefins via Radical-Triggered 1, 2-Alkynyl Migration. Chinese Journal of Organic Chemistry, 2020, 40(2): 423-431. doi: 10.6023/cjoc201909007.","citationCn":"Zhang Ping, Shi Haonan, Zhang Tianshu, Cai Peijun, Jiang Bo, Tu Shujiang. 利用自由基引发的1, 2-炔基迁移实现非活性烯烃的炔膦酰化. 有机化学, 2020, 40(2): 423-431. doi: 10.6023/cjoc201909007.","citationEn":"Zhang Ping, Shi Haonan, Zhang Tianshu, Cai Peijun, Jiang Bo, Tu Shujiang. Alkynylphosphonation of Unactivated Olefins via Radical-Triggered 1, 2-Alkynyl Migration. Chinese Journal of Organic Chemistry, 2020, 40(2): 423-431. doi: 10.6023/cjoc201909007.","doi":"10.6023/cjoc201909007","figContent":"yjhx-40-2-423-S1.jpg$$yjhx-40-2-423-S2.jpg$$yjhx-40-2-423-S3.jpg","figList":["yjhx-40-2-423-S1.jpg","yjhx-40-2-423-S2.jpg","yjhx-40-2-423-S3.jpg"],"firstFig":"yjhx-40-2-423-S1.jpg","fpage":"423","highCitedState":"","htmlCount":164,"htmlFile":"","id":"a3b8ba7a-f186-4777-b431-a63d70390c69","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"1, 4-enynes, alkynylphosphonation, <i>γ<\/i>-ketophosphine oxides, alkynyl migration, radical chemistry","keywordCn":"1, 4-烯炔衍生物, 炔膦酰化反应, <i>γ<\/i>-酮膦氧化物, 炔基迁移, 自由基化学","keywordCnList":["1"," 4-烯炔衍生物"," 炔膦酰化反应"," <i>γ<\/i>-酮膦氧化物"," 炔基迁移"," 自由基化学"],"keywordEn":"1, 4-enynes, alkynylphosphonation, <i>γ<\/i>-ketophosphine oxides, alkynyl migration, radical chemistry","keywordEnList":["1"," 4-enynes"," alkynylphosphonation"," <i>γ<\/i>-ketophosphine oxides"," alkynyl migration"," radical chemistry"],"keywordList":["1"," 4-enynes"," alkynylphosphonation"," <i>γ<\/i>-ketophosphine oxides"," alkynyl migration"," radical chemistry"],"language":"en","latestInfo":"","latestState":"","latestStateEn":"","lpage":"431","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":11,"pdfSize":517.22,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"Alkynylphosphonation of Unactivated Olefins via Radical-Triggered 1, 2-Alkynyl Migration","titleCn":"利用自由基引发的1, 2-炔基迁移实现非活性烯烃的炔膦酰化","titleEn":"Alkynylphosphonation of Unactivated Olefins via Radical-Triggered 1, 2-Alkynyl Migration","viewCount":2000,"volume":"40","year":2020},{"abstractInfo":"Twoseriesofnovelchrysinderivativesweresynthesized,andtheirantiproliferativeactivitywasevaluatedagainstsixhumancancercelllines(MGC-803,BEL-7402,HepG2,HeLa,A549,andSGC-7901)usingmethylthiazolyltetrazolium(MTT)assay.Preliminarybioassayresultsindicatedthat7-((1-(3-fluorophenyl)-1<i>H<\/i>-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4<i>H<\/i>-chromen-4-one(<b>1c<\/b>)and7-((1-(2-chlorophenyl)-1<i>H<\/i>-1,2,3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4<i>H<\/i>-chro-men-4-one(<b>1g<\/b>)exhibitedsignificantlyimprovedantiproliferativeactivitiesagainsttheMGC-803celllinewhencomparedwiththeparentcompoundchrysinandthepositivecontroldrug5-fluorouracil.Itdemonstratesthatcompounds<b>1c<\/b>and<b>1g<\/b>arepotentialagentsforcancertherapy.","abstractInfoCn":"合成了2个系列的白杨素衍生物，采用噻唑蓝（MTT）法测试了所有化合物针对六种肿瘤细胞的体外抗增殖活性，包括MGC-803，BEL-7402，HepG2，HeLa，A549以及SGC-7901细胞.实验结果显示，7-[1-（3-氟苯基）-1<i>H<\/i>-1，2，3-三唑-4-甲氧基]-白杨素（<b>1c<\/b>）与7-[1-（2-氯苯基）-1<i>H<\/i>-1，2，3-三唑-4-甲氧基]-白杨素（<b>1g<\/b>）针对MGC-803细胞的活性与先导化合物白杨素及阳性对照药5-氟尿嘧啶相比显著提高.因此，化合物<b>1c<\/b>与<b>1g<\/b>具有深入研究用以开发抗癌药物的潜能.","abstractInfoEn":"Two series of novel chrysin derivatives were synthesized, and their antiproliferative activity was evaluated against six human cancer cell lines (MGC-803, BEL-7402, HepG2, HeLa, A549, and SGC-7901) using methyl thiazolyl tetrazolium (MTT) assay. Preliminary bioassay results indicated that 7-((1-(3-fluorophenyl)-1<i>H<\/i>-1, 2, 3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4<i>H<\/i>-chromen-4-one (<b>1c<\/b>) and 7-((1-(2-chlorophenyl)-1<i>H<\/i>-1, 2, 3-triazol-4-yl)methoxy)-5-hydroxy-2-phenyl-4<i>H<\/i>-chro-men-4-one (<b>1g<\/b>) exhibited significantly improved antiproliferative activities against the MGC-803 cell line when compared with the parent compound chrysin and the positive control drug 5-fluorouracil. It demonstrates that compounds <b>1c<\/b> and <b>1g<\/b> are potential agents for cancer therapy.","articleNo":"","authorCnList":["栾天"," 全哲山"," 方应权"," 杨宏静"],"authorEnList":["Luan Tian"," Quan Zheshan"," Fang Yingquan"," Yang Hongjing"],"authorList":["Luan Tian"," Quan Zheshan"," Fang Yingquan"," Yang Hongjing"],"authors":"Luan Tian, Quan Zheshan, Fang Yingquan, Yang Hongjing","authorsCn":"栾天, 全哲山, 方应权, 杨宏静","authorsEn":"Luan Tian, Quan Zheshan, Fang Yingquan, Yang Hongjing","categoryName":"Articles","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"Luan Tian, Quan Zheshan, Fang Yingquan, Yang Hongjing. Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties. Chinese Journal of Organic Chemistry, 2020, 40(2): 440-446. doi: 10.6023/cjoc201907012.","citationCn":"Luan Tian, Quan Zheshan, Fang Yingquan, Yang Hongjing. 三唑类白杨素衍生物的设计、合成及其抗增殖活性研究. 有机化学, 2020, 40(2): 440-446. doi: 10.6023/cjoc201907012.","citationEn":"Luan Tian, Quan Zheshan, Fang Yingquan, Yang Hongjing. Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties. Chinese Journal of Organic Chemistry, 2020, 40(2): 440-446. doi: 10.6023/cjoc201907012.","doi":"10.6023/cjoc201907012","figContent":"yjhx-40-2-440-1.jpg$$yjhx-40-2-440-S1.jpg","figList":["yjhx-40-2-440-1.jpg","yjhx-40-2-440-S1.jpg"],"firstFig":"yjhx-40-2-440-1.jpg","fpage":"440","highCitedState":"","htmlCount":207,"htmlFile":"","id":"2f9d2e8e-3f9e-4c6a-ada1-c587f3462d22","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"chrysin, synthesis, triazole, derivatives, antiproliferation","keywordCn":"白杨素, 合成, 三唑, 衍生物, 抗增殖","keywordCnList":["白杨素"," 合成"," 三唑"," 衍生物"," 抗增殖"],"keywordEn":"chrysin, synthesis, triazole, derivatives, antiproliferation","keywordEnList":["chrysin"," synthesis"," triazole"," derivatives"," antiproliferation"],"keywordList":["chrysin"," synthesis"," triazole"," derivatives"," antiproliferation"],"language":"en","latestInfo":"","latestState":"","latestStateEn":"","lpage":"446","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":25,"pdfSize":436.16,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties","titleCn":"三唑类白杨素衍生物的设计、合成及其抗增殖活性研究","titleEn":"Design, Synthesis and Antiproliferative Activity of Chrysin Derivatives Bearing Triazole Moieties","viewCount":2239,"volume":"40","year":2020}],"研究论文":[{"abstractInfo":"报道了一类新颖的醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应.该反应利用醋酸碘苯与<i>N<\/i>-羟基邻苯二甲酰亚胺（或<i>N<\/i>-羟基丁二甲酰亚胺）反应能产生氧中心自由基的特性实现了氧中心自由基诱导的<i>α<\/i>-重氮羰基化合物的双氧合反应，合成了一系列<i>α<\/i>，<i>α<\/i>-双氧代芳酮和<i>α<\/i>，<i>α<\/i>-双氧代羧酸酯衍生物，产率中等到良好.基于实验结果及文献报道，提出了可能的反应机理，其涉及氧中心自由基加成、C-N键的均裂和自由基交叉偶联等.此外，该反应具有无需金属催化剂、条件温和、操作简便等优点.","abstractInfoCn":"报道了一类新颖的醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应.该反应利用醋酸碘苯与<i>N<\/i>-羟基邻苯二甲酰亚胺（或<i>N<\/i>-羟基丁二甲酰亚胺）反应能产生氧中心自由基的特性实现了氧中心自由基诱导的<i>α<\/i>-重氮羰基化合物的双氧合反应，合成了一系列<i>α<\/i>，<i>α<\/i>-双氧代芳酮和<i>α<\/i>，<i>α<\/i>-双氧代羧酸酯衍生物，产率中等到良好.基于实验结果及文献报道，提出了可能的反应机理，其涉及氧中心自由基加成、C-N键的均裂和自由基交叉偶联等.此外，该反应具有无需金属催化剂、条件温和、操作简便等优点.","abstractInfoEn":"A new PhI(OAc)<sub>2<\/sub>-mediated dediazodioxygenation of <i>α<\/i>-diazo carbonyls was reported. By using the characteristics of the <i>in-situ<\/i>-generated <i>O<\/i>-centered radicals from the interaction of PhI(OAc)<sub>2<\/sub> and <i>N<\/i>-hydroxy phthalimide (or <i>N<\/i>-hydroxy succinimide), <i>O<\/i>-centered radical-triggered dioxygenation of <i>α-<\/i>diazo carbonyls was achieved in this transformation, which led to the synthesis of a series of <i>α<\/i>, <i>α<\/i>-dioxoarylketones and <i>α<\/i>, <i>α<\/i>-dioxoesters with moderate to good yields. Based on the experimental results and literature reports, the possible reaction mechanism was proposed, which involved <i>O<\/i>-centered radical addition, C-N bond homolysis and radical cross coupling. In addition, the reaction featured mild conditions and simple operation without any catalyst.","articleNo":"","authorCnList":["李庆雪"," 李梦伟"," 时绍青"," 季晓霜"," 何春兰"," 姜波"," 郝文娟"],"authorEnList":["Li Qingxue"," Li Mengwei"," Shi Shaoqing"," Ji Xiaoshuang"," He Chunlan"," Jiang Bo"," Hao Wenjuan"],"authorList":["李庆雪"," 李梦伟"," 时绍青"," 季晓霜"," 何春兰"," 姜波"," 郝文娟"],"authors":"李庆雪, 李梦伟, 时绍青, 季晓霜, 何春兰, 姜波, 郝文娟","authorsCn":"李庆雪, 李梦伟, 时绍青, 季晓霜, 何春兰, 姜波, 郝文娟","authorsEn":"Li Qingxue, Li Mengwei, Shi Shaoqing, Ji Xiaoshuang, He Chunlan, Jiang Bo, Hao Wenjuan","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"李庆雪, 李梦伟, 时绍青, 季晓霜, 何春兰, 姜波, 郝文娟. 醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应. 有机化学, 2020, 40(2): 384-390. doi: 10.6023/cjoc201909041.","citationCn":"李庆雪, 李梦伟, 时绍青, 季晓霜, 何春兰, 姜波, 郝文娟. 醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应. 有机化学, 2020, 40(2): 384-390. doi: 10.6023/cjoc201909041.","citationEn":"李庆雪, 李梦伟, 时绍青, 季晓霜, 何春兰, 姜波, 郝文娟. PhI(OAc)<sub>2<\/sub>-Mediated Dediazodioxygenation of <i>α<\/i>-Diazo Carbonyls. Chinese Journal of Organic Chemistry, 2020, 40(2): 384-390. doi: 10.6023/cjoc201909041.","doi":"10.6023/cjoc201909041","figContent":"yjhx-40-2-384-S1.jpg$$yjhx-40-2-384-1.jpg$$yjhx-40-2-384-S2.jpg$$yjhx-40-2-384-S3.jpg","figList":["yjhx-40-2-384-S1.jpg","yjhx-40-2-384-1.jpg","yjhx-40-2-384-S2.jpg","yjhx-40-2-384-S3.jpg"],"firstFig":"yjhx-40-2-384-S1.jpg","fpage":"384","highCitedState":"","htmlCount":477,"htmlFile":"","id":"f07e3a16-81ed-49b3-8dcd-75fac0ef20a6","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"双氧合反应, 去重氮化反应, <i>α<\/i>, <i>α<\/i>-双氧代芳酮, <i>α<\/i>, <i>α<\/i>-双氧代羧酸酯","keywordCn":"双氧合反应, 去重氮化反应, <i>α<\/i>, <i>α<\/i>-双氧代芳酮, <i>α<\/i>, <i>α<\/i>-双氧代羧酸酯","keywordCnList":["双氧合反应"," 去重氮化反应"," <i>α<\/i>"," <i>α<\/i>-双氧代芳酮"," <i>α<\/i>"," <i>α<\/i>-双氧代羧酸酯"],"keywordEn":"dioxygenation, dediazotization, <i>α<\/i>, <i>α<\/i>-dioxoarylketones, <i>α<\/i>, <i>α<\/i>-dioxoesters","keywordEnList":["dioxygenation"," dediazotization"," <i>α<\/i>"," <i>α<\/i>-dioxoarylketones"," <i>α<\/i>"," <i>α<\/i>-dioxoesters"],"keywordList":["双氧合反应"," 去重氮化反应"," <i>α<\/i>"," <i>α<\/i>-双氧代芳酮"," <i>α<\/i>"," <i>α<\/i>-双氧代羧酸酯"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"390","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":28,"pdfSize":765.11,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应","titleCn":"醋酸碘苯介导的<i>α<\/i>-重氮羰基化合物的去重氮双氧合反应","titleEn":"PhI(OAc)<sub>2<\/sub>-Mediated Dediazodioxygenation of <i>α<\/i>-Diazo Carbonyls","viewCount":2840,"volume":"40","year":2020},{"abstractInfo":"利用药物设计中的生物活性基团拼接原理，设计合成了13个含吲哚的吡唑并[3，4-<i>d<\/i>]嘧啶衍生物.目标化合物均经核磁共振氢谱（<sup>1<\/sup>HNMR）、核磁共振碳谱（<sup>13<\/sup>CNMR）和高分辨质谱仪（HRMS）进行了结构确证.对4株肿瘤细胞（HeLa、MGC-803、MCF-7、BEL-7404）的体外抗增殖活性实验结果表明，目标化合物均表现出一定的抗肿瘤活性，MCF-7、MGC-803肿瘤细胞株敏感度高于HeLa和BEL-7404.其中，6-[（6-甲氧羰基吲哚-3-基）硫基]-1-苯基-吡唑并[3，4-<i>d<\/i>]嘧啶-4-酮（<b>5m<\/b>）表现出较好的体外肿瘤抑制活性，对MCF-7、MGC-80和HeLa细胞的IC<sub>50<\/sub>均小于30μmol·L<sup>-1<\/sup>，对MCF-7的IC<sub>50<\/sub>值为（4.02±0.92）μmol·L<sup>-1<\/sup>，优于对照药物依托泊苷（10.1±0.62μmol·L<sup>-1<\/sup>）和羟喜树碱（5.93±0.56μmol·L<sup>-1<\/sup>）.拓扑异构酶抑制实验结果表明，此类化合物对TopoⅡ有选择性抑制活性，所有化合物对TopoⅡ表现出不同程度抑制活性，对TopoⅠ未表现出抑制活性.","abstractInfoCn":"利用药物设计中的生物活性基团拼接原理，设计合成了13个含吲哚的吡唑并[3，4-<i>d<\/i>]嘧啶衍生物.目标化合物均经核磁共振氢谱（<sup>1<\/sup>H NMR）、核磁共振碳谱（<sup>13<\/sup>C NMR）和高分辨质谱仪（HRMS）进行了结构确证.对4株肿瘤细胞（HeLa、MGC-803、MCF-7、BEL-7404）的体外抗增殖活性实验结果表明，目标化合物均表现出一定的抗肿瘤活性，MCF-7、MGC-803肿瘤细胞株敏感度高于HeLa和BEL-7404.其中，6-[（6-甲氧羰基吲哚-3-基）硫基]-1-苯基-吡唑并[3，4-<i>d<\/i>]嘧啶-4-酮（<b>5m<\/b>）表现出较好的体外肿瘤抑制活性，对MCF-7、MGC-80和HeLa细胞的IC<sub>50<\/sub>均小于30 μmol·L<sup>-1<\/sup>，对MCF-7的IC<sub>50<\/sub>值为（4.02±0.92）μmol·L<sup>-1<\/sup>，优于对照药物依托泊苷（10.1±0.62 μmol·L<sup>-1<\/sup>）和羟喜树碱（5.93±0.56 μmol·L<sup>-1<\/sup>）.拓扑异构酶抑制实验结果表明，此类化合物对Topo Ⅱ有选择性抑制活性，所有化合物对Topo Ⅱ表现出不同程度抑制活性，对Topo Ⅰ未表现出抑制活性.","abstractInfoEn":"Based on the combination principle in drug design, thirteen pyrazolo[3, 4-<i>d<\/i>]pyrimidine derivatives containing indole moiety were designed and synthesized. The target compounds were confirmed by <sup>1<\/sup>H NMR, <sup>13<\/sup>C NMR and HRMS. Their <i>in vitro<\/i> cytotoxicity against four human cancer cell lines (HeLa、MGC-803、MCF-7、BEL-7404) has been investigated and most of the tested compounds displayed moderate antiproliferative activity. Especially, compound <b>5m<\/b> exhibited the highest level of antiproliferative activity with an IC<sub>50<\/sub> value &lt; 30 μmol·L<sup>-1<\/sup> for HeLa, MGC-803 and MCF-7. IC<sub>50<\/sub> value of methyl 3-((4-oxo-1-phenyl-4, 5-dihydro-1<i>H<\/i>-pyrazolo[3, 4-d]pyrimidin-6-yl)thio)-1<i>H<\/i>-indole-6-carboxylate (<b>5m<\/b>) to MCF-7 was (4.02±0.92) μmol·L<sup>-1<\/sup>, which was better than etoposide (10.1±0.62 μmol·L<sup>-1<\/sup>) and camptothecin (5.93±0.56 μmol·L<sup>-1<\/sup>). Further biological evaluation of these compounds suggested that these compounds showed selective inhibitory activity against Topo Ⅱ as a possible intracellular target, and all compounds didn't show inhibitory activity against Topo Ⅰ.","articleNo":"","authorCnList":["孙晓阳"," 冯思冉"," 董金娇"," 冯佳佳"," 刘振明"," 宋亚丽"," 乔晓强"],"authorEnList":["Sun Xiaoyang"," Feng Siran"," Dong Jinjiao"," Feng Jiajia"," Liu Zhenming"," Song Yali"," Qiao Xiaoqiang"],"authorList":["孙晓阳"," 冯思冉"," 董金娇"," 冯佳佳"," 刘振明"," 宋亚丽"," 乔晓强"],"authors":"孙晓阳, 冯思冉, 董金娇, 冯佳佳, 刘振明, 宋亚丽, 乔晓强","authorsCn":"孙晓阳, 冯思冉, 董金娇, 冯佳佳, 刘振明, 宋亚丽, 乔晓强","authorsEn":"Sun Xiaoyang, Feng Siran, Dong Jinjiao, Feng Jiajia, Liu Zhenming, Song Yali, Qiao Xiaoqiang","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"孙晓阳, 冯思冉, 董金娇, 冯佳佳, 刘振明, 宋亚丽, 乔晓强. 含吲哚的吡唑并[3, 4-<i>d<\/i>]嘧啶衍生物的设计合成及其生物活性研究. 有机化学, 2020, 40(2): 391-397. doi: 10.6023/cjoc201907006.","citationCn":"孙晓阳, 冯思冉, 董金娇, 冯佳佳, 刘振明, 宋亚丽, 乔晓强. 含吲哚的吡唑并[3, 4-<i>d<\/i>]嘧啶衍生物的设计合成及其生物活性研究. 有机化学, 2020, 40(2): 391-397. doi: 10.6023/cjoc201907006.","citationEn":"孙晓阳, 冯思冉, 董金娇, 冯佳佳, 刘振明, 宋亚丽, 乔晓强. Design, Synthesis and Biological Activity of Pyrazolo[3, 4-<i>d<\/i>]pyrimidine Derivatives Containing Indole Moiety. Chinese Journal of Organic Chemistry, 2020, 40(2): 391-397. doi: 10.6023/cjoc201907006.","doi":"10.6023/cjoc201907006","figContent":"yjhx-40-2-391-1.jpg$$yjhx-40-2-391-S1.jpg$$yjhx-40-2-391-2.jpg$$yjhx-40-2-391-3.jpg$$yjhx-40-2-391-4.jpg$$yjhx-40-2-391-5.jpg$$yjhx-40-2-391-6.jpg","figList":["yjhx-40-2-391-1.jpg","yjhx-40-2-391-S1.jpg","yjhx-40-2-391-2.jpg","yjhx-40-2-391-3.jpg","yjhx-40-2-391-4.jpg","yjhx-40-2-391-5.jpg","yjhx-40-2-391-6.jpg"],"firstFig":"yjhx-40-2-391-1.jpg","fpage":"391","highCitedState":"","htmlCount":457,"htmlFile":"","id":"3d807520-d1d5-499f-a683-aa8cc48396bf","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"吲哚, 吡唑并[3, 4-<i>d<\/i>]嘧啶, 抗肿瘤, 拓扑异构酶, 分子对接","keywordCn":"吲哚, 吡唑并[3, 4-<i>d<\/i>]嘧啶, 抗肿瘤, 拓扑异构酶, 分子对接","keywordCnList":["吲哚"," 吡唑并[3"," 4-<i>d<\/i>]嘧啶"," 抗肿瘤"," 拓扑异构酶"," 分子对接"],"keywordEn":"indole, pyrazolo[3, 4-<i>d<\/i>]pyrimidine, anticancer, topoisomerase, molecular docking","keywordEnList":["indole"," pyrazolo[3"," 4-<i>d<\/i>]pyrimidine"," anticancer"," topoisomerase"," molecular docking"],"keywordList":["吲哚"," 吡唑并[3"," 4-<i>d<\/i>]嘧啶"," 抗肿瘤"," 拓扑异构酶"," 分子对接"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"397","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":19,"pdfSize":1054.72,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"含吲哚的吡唑并[3, 4-<i>d<\/i>]嘧啶衍生物的设计合成及其生物活性研究","titleCn":"含吲哚的吡唑并[3, 4-<i>d<\/i>]嘧啶衍生物的设计合成及其生物活性研究","titleEn":"Design, Synthesis and Biological Activity of Pyrazolo[3, 4-<i>d<\/i>]pyrimidine Derivatives Containing Indole Moiety","viewCount":2805,"volume":"40","year":2020},{"abstractInfo":"设计合成了三类含1，2，3-三氮唑结构的1，5-苯并硫氮杂（艹卓）化合物3-（1<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，5-二氢-1，5-苯并硫氮杂（艹卓）（<b>5a<\/b>~<b>5f<\/b>）、3-（2<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，3-二氢-1，5-苯并硫氮杂（艹卓）（<b>6a<\/b>~<b>6f<\/b>）和3-（1<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，3，4，5-四氢-1，5-苯并硫氮杂（艹卓）（<b>7a<\/b>~<b>7f<\/b>）.研究了中间体及目标产物的合成条件，分离出其中两个副产物并进行了结构确定.目标产物的抑真菌活性测试表明，化合物<b>5a<\/b>~<b>5f<\/b>对真菌具有良好的抑制作用，对新生隐球菌的抑制效果尤为突出.初步抑真菌构效关系研究表明，1<i>H<\/i>-1，2，3-三氮唑环和C=C双键是化合物<b>5a<\/b>~<b>5f<\/b>抑真菌活性的关键官能团.","abstractInfoCn":"设计合成了三类含1，2，3-三氮唑结构的1，5-苯并硫氮杂（艹卓）化合物3-（1<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，5-二氢-1，5-苯并硫氮杂（艹卓）（<b>5a<\/b>~<b>5f<\/b>）、3-（2<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，3-二氢-1，5-苯并硫氮杂（艹卓）（<b>6a<\/b>~<b>6f<\/b>）和3-（1<i>H<\/i>-1，2，3-三氮唑）-4-芳基-2，3，4，5-四氢-1，5-苯并硫氮杂（艹卓）（<b>7a<\/b>~<b>7f<\/b>）.研究了中间体及目标产物的合成条件，分离出其中两个副产物并进行了结构确定.目标产物的抑真菌活性测试表明，化合物<b>5a<\/b>~<b>5f<\/b>对真菌具有良好的抑制作用，对新生隐球菌的抑制效果尤为突出.初步抑真菌构效关系研究表明，1<i>H<\/i>-1，2，3-三氮唑环和C=C双键是化合物<b>5a<\/b>~<b>5f<\/b>抑真菌活性的关键官能团.","abstractInfoEn":"Three kinds of 1, 5-benzothiazepines containing 1, 2, 3-triazole, 3-(1<i>H<\/i>-1, 2, 3-triazolyl)-4-aryl-2, 5-dihydro-1, 5-benzo-thiazepines (<b>5a<\/b>~<b>5f<\/b>), 3-(2<i>H<\/i>-1, 2, 3-triazolyl)-4-aryl-2, 3-dihydro-1, 5-benzothiazepines (<b>6a<\/b>~<b>6f<\/b>) and 3-(1<i>H<\/i>-1, 2, 3-triazolyl)-4-aryl-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepines (<b>7a<\/b>~<b>7f<\/b>), were designed and synthesized. The synthesis conditions of intermediates and target products were studied. Two by-products were separated and their structures were determined. The antifungal activity test of the target products showed that compounds <b>5a<\/b>~<b>5f<\/b> exhibited high inhibitory effects against fungi especially for <i>Cryptococcus neoformans<\/i>. The preliminary study on the structure-activity relationship of antifungal activity reveled that 1<i>H<\/i>-1, 2, 3-triazolyl and C=C double bond were the key function groups in the antifungal activity of <b>5a<\/b>~<b>5f<\/b>.","articleNo":"","authorCnList":["王冉冉"," 王岩"," 边彦青"," 张萍"],"authorEnList":["Wang Ranran"," Wang Yan"," Bian Yanqing"," Zhang Ping"],"authorList":["王冉冉"," 王岩"," 边彦青"," 张萍"],"authors":"王冉冉, 王岩, 边彦青, 张萍","authorsCn":"王冉冉, 王岩, 边彦青, 张萍","authorsEn":"Wang Ranran, Wang Yan, Bian Yanqing, Zhang Ping","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"王冉冉, 王岩, 边彦青, 张萍. 含1, 2, 3-三氮唑结构的1, 5-苯并硫氮杂（艹卓）的合成及其抑真菌活性. 有机化学, 2020, 40(2): 398-407. doi: 10.6023/cjoc201907056.","citationCn":"王冉冉, 王岩, 边彦青, 张萍. 含1, 2, 3-三氮唑结构的1, 5-苯并硫氮杂（艹卓）的合成及其抑真菌活性. 有机化学, 2020, 40(2): 398-407. doi: 10.6023/cjoc201907056.","citationEn":"王冉冉, 王岩, 边彦青, 张萍. Synthesis and Antifungal Activity of 1, 5-Benzothiazepines Containing 1, 2, 3-Triazole. Chinese Journal of Organic Chemistry, 2020, 40(2): 398-407. doi: 10.6023/cjoc201907056.","doi":"10.6023/cjoc201907056","figContent":"yjhx-40-2-398-S1.jpg$$yjhx-40-2-398-1.jpg","figList":["yjhx-40-2-398-S1.jpg","yjhx-40-2-398-1.jpg"],"firstFig":"yjhx-40-2-398-S1.jpg","fpage":"398","highCitedState":"","htmlCount":378,"htmlFile":"","id":"f537dbbf-b04b-4f8c-8b08-6fd8bd69c1ba","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"1, 5-苯并硫氮杂, 1, 2, 3-三氮唑, 抑真菌活性, 构效关系","keywordCn":"1, 5-苯并硫氮杂, 1, 2, 3-三氮唑, 抑真菌活性, 构效关系","keywordCnList":["1"," 5-苯并硫氮杂"," 1"," 2"," 3-三氮唑"," 抑真菌活性"," 构效关系"],"keywordEn":"1, 5-benzothiazepine, 1, 2, 3-triazole, antifungal activity, structure-activity relationship","keywordEnList":["1"," 5-benzothiazepine"," 1"," 2"," 3-triazole"," antifungal activity"," structure-activity relationship"],"keywordList":["1"," 5-苯并硫氮杂"," 1"," 2"," 3-三氮唑"," 抑真菌活性"," 构效关系"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"407","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":17,"pdfSize":722.06,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"含1, 2, 3-三氮唑结构的1, 5-苯并硫氮杂（艹卓）的合成及其抑真菌活性","titleCn":"含1, 2, 3-三氮唑结构的1, 5-苯并硫氮杂（艹卓）的合成及其抑真菌活性","titleEn":"Synthesis and Antifungal Activity of 1, 5-Benzothiazepines Containing 1, 2, 3-Triazole","viewCount":2856,"volume":"40","year":2020},{"abstractInfo":"香豆素和吡唑并[3，4-<i>b<\/i>]吡啶骨架广泛存在于具有生物活性的天然化合物中，在药物化学中也被广泛用作药物核心单元，具有极其重要的作用.以磷酸改性铌酸作为催化剂，通过微波辐射下醛、香豆素衍生物、5-氨基吡唑的三组分反应一锅法高产率地合成一系列香豆素修饰的吡唑并[3，4-<i>b<\/i>]吡啶衍生物.该反应一步完成，具有催化剂和溶剂对环境友好，操作简单等优点.产物的结构经红外光谱、核磁共振谱及高分辨质谱予以确定.","abstractInfoCn":"香豆素和吡唑并[3，4-<i>b<\/i>]吡啶骨架广泛存在于具有生物活性的天然化合物中，在药物化学中也被广泛用作药物核心单元，具有极其重要的作用.以磷酸改性铌酸作为催化剂，通过微波辐射下醛、香豆素衍生物、5-氨基吡唑的三组分反应一锅法高产率地合成一系列香豆素修饰的吡唑并[3，4-<i>b<\/i>]吡啶衍生物.该反应一步完成，具有催化剂和溶剂对环境友好，操作简单等优点.产物的结构经红外光谱、核磁共振谱及高分辨质谱予以确定.","abstractInfoEn":"Coumarin and pyrazolo[3, 4-<i>b<\/i>]pyridine are structurally essential elements in biologically active natural compounds and are extremely important in medicinal chemistry by serving as key pharmacophores in drug discovery. In this article, the efficient synthesis of coumarin-fused pyrazolo[3, 4-<i>b<\/i>]pyridine via three-component domino reaction of aldehydes, coumarin derivative and 5-aminopyrazole in one step catalyzed by niobic acid modified with phosphoric acid under microwave irradiation has been achieved. The one-pot procedure, eco-friendly catalyst and solvent as well as simple operation are the key features of this method. The structures of the products were identified by IR, NMR, and HRMS spectra.","articleNo":"","authorCnList":["林伟"," 庄苍伟"," 胡秀秀"," 杨凤丽"],"authorEnList":["Lin Wei"," Zhuang Cangwei"," Hu Xiuxiu"," Yang Fengli"],"authorList":["林伟"," 庄苍伟"," 胡秀秀"," 杨凤丽"],"authors":"林伟, 庄苍伟, 胡秀秀, 杨凤丽","authorsCn":"林伟, 庄苍伟, 胡秀秀, 杨凤丽","authorsEn":"Lin Wei, Zhuang Cangwei, Hu Xiuxiu, Yang Fengli","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"林伟, 庄苍伟, 胡秀秀, 杨凤丽. 微波辐射下磷酸改性铌酸催化的香豆素修饰吡唑并[3, 4-<i>b<\/i>]吡啶衍生物的高效合成. 有机化学, 2020, 40(2): 408-416. doi: 10.6023/cjoc201907026.","citationCn":"林伟, 庄苍伟, 胡秀秀, 杨凤丽. 微波辐射下磷酸改性铌酸催化的香豆素修饰吡唑并[3, 4-<i>b<\/i>]吡啶衍生物的高效合成. 有机化学, 2020, 40(2): 408-416. doi: 10.6023/cjoc201907026.","citationEn":"林伟, 庄苍伟, 胡秀秀, 杨凤丽. Efficient Synthesis of Coumarin-Fused Pyrazolo[3, 4-<i>b<\/i>]pyridine Derivatives Catalyzed by Niobic Acid Modified with Phosphoric Acid under Microwave Irradiation. Chinese Journal of Organic Chemistry, 2020, 40(2): 408-416. doi: 10.6023/cjoc201907026.","doi":"10.6023/cjoc201907026","figContent":"yjhx-40-2-408-1.jpg$$yjhx-40-2-408-2.jpg$$yjhx-40-2-408-S1.jpg$$yjhx-40-2-408-S2.jpg","figList":["yjhx-40-2-408-1.jpg","yjhx-40-2-408-2.jpg","yjhx-40-2-408-S1.jpg","yjhx-40-2-408-S2.jpg"],"firstFig":"yjhx-40-2-408-1.jpg","fpage":"408","highCitedState":"","htmlCount":278,"htmlFile":"","id":"edada4cc-a056-4bcc-9656-1c57f16b312c","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"香豆素, 吡唑并[3, 4-<i>b<\/i>]吡啶, 合成, 铌酸","keywordCn":"香豆素, 吡唑并[3, 4-<i>b<\/i>]吡啶, 合成, 铌酸","keywordCnList":["香豆素"," 吡唑并[3"," 4-<i>b<\/i>]吡啶"," 合成"," 铌酸"],"keywordEn":"coumarin, pyrazolo[3, 4-<i>b<\/i>]pyridine, synthesis, niobic acid","keywordEnList":["coumarin"," pyrazolo[3"," 4-<i>b<\/i>]pyridine"," synthesis"," niobic acid"],"keywordList":["香豆素"," 吡唑并[3"," 4-<i>b<\/i>]吡啶"," 合成"," 铌酸"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"416","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":7,"pdfSize":852.24,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"微波辐射下磷酸改性铌酸催化的香豆素修饰吡唑并[3, 4-<i>b<\/i>]吡啶衍生物的高效合成","titleCn":"微波辐射下磷酸改性铌酸催化的香豆素修饰吡唑并[3, 4-<i>b<\/i>]吡啶衍生物的高效合成","titleEn":"Efficient Synthesis of Coumarin-Fused Pyrazolo[3, 4-<i>b<\/i>]pyridine Derivatives Catalyzed by Niobic Acid Modified with Phosphoric Acid under Microwave Irradiation","viewCount":2401,"volume":"40","year":2020},{"abstractInfo":"细胞分裂周期25磷酸酯酶B（Cdc25B）与致癌转化有关，是潜在的抗癌疗法的药物靶标.为筛选Cdc25B抑制剂，以1，3-硒唑为核心组块，利用酰胺硫醚键与1，2，4-三唑席夫碱活性组块桥连成目标化合物2-（1，2，4-三唑-3-基）硫代-<i>N<\/i>-（4-苯基-1，3-硒唑-2-基）乙酰胺（<b>TATS<\/b>）.首先为验证将1，3-硒唑作为核心组块的合理性，选择了苯环未被修饰的<b>TATS1<\/b>与Cdc25B进行分子对接模拟，结果表明，1，3-硒唑能紧密地嵌入Cdc25B结构中，与Cdc25B的重要催化位点Arg492发生N-H…PI非键弱相互作用，发挥了核心作用.酰胺羰基氧原子与Arg492和Arg488形成氢键，表明酰胺硫醚键引入合理.在理论对接研究的基础上，通过对1，2，4-三唑席夫碱活性组块中两个区域用不同基团修饰，设计并合成了13个新型目标化合物<b>TATS1<\/b>~<b>TATS13<\/b>，对比测试了目标化合物和重要中间体对Cdc25B的抑制活性.结果表明，其中12个目标化合物生物活性优于阳性参照物Na<sub>3<\/sub>VO<sub>4<\/sub>，1，2，4-三唑席夫碱两个区域的不同修饰对抑制活性有明显影响，实现了活性叠加效应，表明该类结构化合物有望成为潜在的Cdc25B抑制剂.","abstractInfoCn":"细胞分裂周期25磷酸酯酶B（Cdc25B）与致癌转化有关，是潜在的抗癌疗法的药物靶标.为筛选Cdc25B抑制剂，以1，3-硒唑为核心组块，利用酰胺硫醚键与1，2，4-三唑席夫碱活性组块桥连成目标化合物2-（1，2，4-三唑-3-基）硫代-<i>N<\/i>-（4-苯基-1，3-硒唑-2-基）乙酰胺（<b>TATS<\/b>）.首先为验证将1，3-硒唑作为核心组块的合理性，选择了苯环未被修饰的<b>TATS1<\/b>与Cdc25B进行分子对接模拟，结果表明，1，3-硒唑能紧密地嵌入Cdc25B结构中，与Cdc25B的重要催化位点Arg492发生N-H…PI非键弱相互作用，发挥了核心作用.酰胺羰基氧原子与Arg492和Arg488形成氢键，表明酰胺硫醚键引入合理.在理论对接研究的基础上，通过对1，2，4-三唑席夫碱活性组块中两个区域用不同基团修饰，设计并合成了13个新型目标化合物<b>TATS1<\/b>~<b>TATS13<\/b>，对比测试了目标化合物和重要中间体对Cdc25B的抑制活性.结果表明，其中12个目标化合物生物活性优于阳性参照物Na<sub>3<\/sub>VO<sub>4<\/sub>，1，2，4-三唑席夫碱两个区域的不同修饰对抑制活性有明显影响，实现了活性叠加效应，表明该类结构化合物有望成为潜在的Cdc25B抑制剂.","abstractInfoEn":"The cell division cycle 25 phosphatase B (Cdc25B) is involved in carcinogenic transformation and is a potential drug target for anticancer therapy. In order to screen Cdc25B inhibitors, 1, 3-selenazole was selected as the core block, and 1, 2, 4-triazole Schiff base was bridged into 2-(1, 2, 4-triazol-3-yl)thio-<i>N<\/i>-(4-phenyl-1, 3-selenazolyl-2-yl)acetamide (<b>TATS<\/b>) by the amide thioether bond. The molecular docking simulation of <b>TATS1<\/b> with Cdc25B was first performed to identify the rationality of the core function of 1, 3-selenazole. The results show that 1, 3-selenazole can be tightly embedded in the Cdc25B structure and perform N-H…PI non-bond weak interaction with the important catalytic site Arg492, which indicates that 1, 3-selenazole plays a central role. The amide carbonyl oxygen atom forms a hydrogen bond with Arg492 and Arg488, indicating that the introduction of the amide thioether bond is reasonable. Based on the theoretical docking study, thirteen new target compounds <b>TATS1<\/b>~<b>TATS13<\/b> were designed and synthesized through modification in two regions of 1, 2, 4-triazole Schiff base. The inhibition against Cdc25B of target molecules and important intermediates was tested respectively. As a result, the inhibitory activities of the intermediates are not good, 12 target compounds have better biological activity than the positive reference substance Na<sub>3<\/sub>VO<sub>4<\/sub>, the modifications of two regions of 1, 2, 4-triazole also have a significant effect, which suggests that these compounds are expected to be a potential inhibitor of Cdc25B.","articleNo":"","authorCnList":["张成路"," 王华玉"," 于向坤"," 杨敬怡"," 李传银"," 宫荣庆"," 宋府璐"," 孙越冬"],"authorEnList":["Zhang Chenglu"," Wang Huayu"," Yu Xiangkun"," Yang Jingyi"," Li Chuanyin"," Gong Rongqin"," Song Fulu"," Sun Yuedong"],"authorList":["张成路"," 王华玉"," 于向坤"," 杨敬怡"," 李传银"," 宫荣庆"," 宋府璐"," 孙越冬"],"authors":"张成路, 王华玉, 于向坤, 杨敬怡, 李传银, 宫荣庆, 宋府璐, 孙越冬","authorsCn":"张成路, 王华玉, 于向坤, 杨敬怡, 李传银, 宫荣庆, 宋府璐, 孙越冬","authorsEn":"Zhang Chenglu, Wang Huayu, Yu Xiangkun, Yang Jingyi, Li Chuanyin, Gong Rongqin, Song Fulu, Sun Yuedong","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"张成路, 王华玉, 于向坤, 杨敬怡, 李传银, 宫荣庆, 宋府璐, 孙越冬. 酰胺硫醚桥连1, 3-硒唑和1, 2, 4-三唑衍生物合成及其对细胞分裂周期25磷酸酯酶B(Cdc25B)抑制活性. 有机化学, 2020, 40(2): 432-439. doi: 10.6023/cjoc201907020.","citationCn":"张成路, 王华玉, 于向坤, 杨敬怡, 李传银, 宫荣庆, 宋府璐, 孙越冬. 酰胺硫醚桥连1, 3-硒唑和1, 2, 4-三唑衍生物合成及其对细胞分裂周期25磷酸酯酶B(Cdc25B)抑制活性. 有机化学, 2020, 40(2): 432-439. doi: 10.6023/cjoc201907020.","citationEn":"张成路, 王华玉, 于向坤, 杨敬怡, 李传银, 宫荣庆, 宋府璐, 孙越冬. Synthesis of Amide Thioether Bridged 1, 3-Selenazole and 1, 2, 4-Triazole Derivatives and Their Inhibitory Activity against Cell Division Cycle Phosphatase B (Cdc25B). Chinese Journal of Organic Chemistry, 2020, 40(2): 432-439. doi: 10.6023/cjoc201907020.","doi":"10.6023/cjoc201907020","figContent":"yjhx-40-2-432-1.jpg$$yjhx-40-2-432-S1.jpg$$yjhx-40-2-432-2.jpg","figList":["yjhx-40-2-432-1.jpg","yjhx-40-2-432-S1.jpg","yjhx-40-2-432-2.jpg"],"firstFig":"yjhx-40-2-432-1.jpg","fpage":"432","highCitedState":"","htmlCount":188,"htmlFile":"","id":"3242b75b-60f5-4c87-be32-b05b34bb04ca","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"1, 3-硒唑, 1, 2, 4-三唑席夫碱, 分子对接模拟, Cdc25B抑制剂","keywordCn":"1, 3-硒唑, 1, 2, 4-三唑席夫碱, 分子对接模拟, Cdc25B抑制剂","keywordCnList":["1"," 3-硒唑"," 1"," 2"," 4-三唑席夫碱"," 分子对接模拟"," Cdc25B抑制剂"],"keywordEn":"1, 3-selenazole, 1, 2, 4-triazole Schiff base, molecular docking simulation, Cdc25B inhibitor","keywordEnList":["1"," 3-selenazole"," 1"," 2"," 4-triazole Schiff base"," molecular docking simulation"," Cdc25B inhibitor"],"keywordList":["1"," 3-硒唑"," 1"," 2"," 4-三唑席夫碱"," 分子对接模拟"," Cdc25B抑制剂"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"439","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":8,"pdfSize":994.47,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"酰胺硫醚桥连1, 3-硒唑和1, 2, 4-三唑衍生物合成及其对细胞分裂周期25磷酸酯酶B(Cdc25B)抑制活性","titleCn":"酰胺硫醚桥连1, 3-硒唑和1, 2, 4-三唑衍生物合成及其对细胞分裂周期25磷酸酯酶B(Cdc25B)抑制活性","titleEn":"Synthesis of Amide Thioether Bridged 1, 3-Selenazole and 1, 2, 4-Triazole Derivatives and Their Inhibitory Activity against Cell Division Cycle Phosphatase B (Cdc25B)","viewCount":2077,"volume":"40","year":2020},{"abstractInfo":"报道了一种用高价碘试剂促进缩氨基硫脲分子内氧化偶联反应，能够有效地合成2-氨基-1，3，4-噻二唑类衍生物.高价碘可以作为温和的反应试剂，拥有毒性低、廉价可循环易操作的特性.该反应具有原料易制得、操作简便以及较好的底物适用性等特点.反应机理也进行了初步研究.","abstractInfoCn":"报道了一种用高价碘试剂促进缩氨基硫脲分子内氧化偶联反应，能够有效地合成2-氨基-1，3，4-噻二唑类衍生物.高价碘可以作为温和的反应试剂，拥有毒性低、廉价可循环易操作的特性.该反应具有原料易制得、操作简便以及较好的底物适用性等特点.反应机理也进行了初步研究.","abstractInfoEn":"A highly method for intramolecular oxidative coupling reaction of thiosemicarbazone promoted by hypervalent iodine reagent was reported. 2-Amino-1, 3, 4-thiadiazole derivatives could be synthesized effectively. Hypervalent iodine could be used as a mild reagent with low toxicity, low cost, easy circulation and operation. The reaction had the advantages of easy preparation of raw materials, simple operation and better performance. The applicability of substrates and the reaction mechanism were also preliminarily studied.","articleNo":"","authorCnList":["陆雨函"," 韩颖芝"," 孙亚栋"," 阿布力米提·阿布都卡德尔"," 王多志"," 刘晨江"],"authorEnList":["Lu Yuhan"," Han Yingzhi"," Sun Yadong"," Abdukader Ablimit"," Wang Duozhi"," Liu Chenjiang"],"authorList":["陆雨函"," 韩颖芝"," 孙亚栋"," 阿布力米提·阿布都卡德尔"," 王多志"," 刘晨江"],"authors":"陆雨函, 韩颖芝, 孙亚栋, 阿布力米提·阿布都卡德尔, 王多志, 刘晨江","authorsCn":"陆雨函, 韩颖芝, 孙亚栋, 阿布力米提·阿布都卡德尔, 王多志, 刘晨江","authorsEn":"Lu Yuhan, Han Yingzhi, Sun Yadong, Abdukader Ablimit, Wang Duozhi, Liu Chenjiang","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"","citation":"陆雨函, 韩颖芝, 孙亚栋, 阿布力米提·阿布都卡德尔, 王多志, 刘晨江. 醋酸碘苯促进的氧化反应在构建2-氨基-1, 3, 4-噻二唑分子中的应用. 有机化学, 2020, 40(2): 447-453. doi: 10.6023/cjoc201907037.","citationCn":"陆雨函, 韩颖芝, 孙亚栋, 阿布力米提·阿布都卡德尔, 王多志, 刘晨江. 醋酸碘苯促进的氧化反应在构建2-氨基-1, 3, 4-噻二唑分子中的应用. 有机化学, 2020, 40(2): 447-453. doi: 10.6023/cjoc201907037.","citationEn":"陆雨函, 韩颖芝, 孙亚栋, 阿布力米提·阿布都卡德尔, 王多志, 刘晨江. Application of Iodobenzene Acetate Promoted Oxidation in the Synthesis of 2-Amino-1, 3, 4-thiadiazole Molecules. Chinese Journal of Organic Chemistry, 2020, 40(2): 447-453. doi: 10.6023/cjoc201907037.","doi":"10.6023/cjoc201907037","figContent":"yjhx-40-2-447-1.jpg$$yjhx-40-2-447-2.jpg$$yjhx-40-2-447-3.jpg$$yjhx-40-2-447-4.jpg","figList":["yjhx-40-2-447-1.jpg","yjhx-40-2-447-2.jpg","yjhx-40-2-447-3.jpg","yjhx-40-2-447-4.jpg"],"firstFig":"yjhx-40-2-447-1.jpg","fpage":"447","highCitedState":"","htmlCount":808,"htmlFile":"","id":"965c80a5-bd1e-459a-991e-ceccca5a31ac","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"高价碘, 氧化, 芳香醛, 噻二唑","keywordCn":"高价碘, 氧化, 芳香醛, 噻二唑","keywordCnList":["高价碘"," 氧化"," 芳香醛"," 噻二唑"],"keywordEn":"hypervalent iodine, oxidation, aromatic aldehydes, thiadiazole","keywordEnList":["hypervalent iodine"," oxidation"," aromatic aldehydes"," thiadiazole"],"keywordList":["高价碘"," 氧化"," 芳香醛"," 噻二唑"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"453","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":32,"pdfSize":613.56,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"醋酸碘苯促进的氧化反应在构建2-氨基-1, 3, 4-噻二唑分子中的应用","titleCn":"醋酸碘苯促进的氧化反应在构建2-氨基-1, 3, 4-噻二唑分子中的应用","titleEn":"Application of Iodobenzene Acetate Promoted Oxidation in the Synthesis of 2-Amino-1, 3, 4-thiadiazole Molecules","viewCount":4003,"volume":"40","year":2020},{"abstractInfo":"8-氨基喹啉的C（5）位碳-氢键氟化反应近年来受到广泛关注，但大多需要使用过渡金属催化剂和亲电氟化试剂来实现.在高价碘试剂的介导下实现了无过渡金属催化条件下的8-氨基喹啉C（5）位碳-氢键亲核氟化反应.使用廉价易得且安全稳定的氟化银作为亲核氟化试剂，反应无需惰性气体保护，条件简单，操作方便，区域选择性好，底物范围较广，为喹啉类化合物的氟化提供了一种有潜在应用价值的新方法.","abstractInfoCn":"8-氨基喹啉的C（5）位碳-氢键氟化反应近年来受到广泛关注，但大多需要使用过渡金属催化剂和亲电氟化试剂来实现.在高价碘试剂的介导下实现了无过渡金属催化条件下的8-氨基喹啉C（5）位碳-氢键亲核氟化反应.使用廉价易得且安全稳定的氟化银作为亲核氟化试剂，反应无需惰性气体保护，条件简单，操作方便，区域选择性好，底物范围较广，为喹啉类化合物的氟化提供了一种有潜在应用价值的新方法.","abstractInfoEn":"The C(5) C-H fluorination of 8-aminoqunolines has attracted much attention recently. However, transition-metal catalyst and electrophilic fluorination reagents were required in most of these reactions. Transition-metal catalyst free C(5) C-H nucleophilic fluorination of 8-aminoqunolines was reviewed. This reaction was mediated by a hypervalent iodine reagent and employed cheap, safe and stable silver fluoride as the nucleophilic fluorination reagent. The reaction proceeded without inert gas protection. It possess the merits of simple and mild reaction conditions, easy operation, high regioselectivity and wide substrate scope and provides a novel method for fluorination of quinolines with potential application value.","articleNo":"","authorCnList":["陈倩雯"," 杨耀成"," 王霞"," 张谦"," 李栋"],"authorEnList":["Chen Qianwen"," Yang Yaocheng"," Wang Xia"," Zhang Qian"," Li Dong"],"authorList":["陈倩雯"," 杨耀成"," 王霞"," 张谦"," 李栋"],"authors":"陈倩雯, 杨耀成, 王霞, 张谦, 李栋","authorsCn":"陈倩雯, 杨耀成, 王霞, 张谦, 李栋","authorsEn":"Chen Qianwen, Yang Yaocheng, Wang Xia, Zhang Qian, Li Dong","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"陈倩雯, 杨耀成, 王霞, 张谦, 李栋. 高价碘试剂介导的8-氨基喹啉C(5)位碳-氢键亲核氟化反应. 有机化学, 2020, 40(2): 454-461. doi: 10.6023/cjoc201907046.","citationCn":"陈倩雯, 杨耀成, 王霞, 张谦, 李栋. 高价碘试剂介导的8-氨基喹啉C(5)位碳-氢键亲核氟化反应. 有机化学, 2020, 40(2): 454-461. doi: 10.6023/cjoc201907046.","citationEn":"陈倩雯, 杨耀成, 王霞, 张谦, 李栋. Hypervalent Iodine Reagent-Mediated C(5) C-H Nucleophilic Fluorination of 8-Aminoqunolines. Chinese Journal of Organic Chemistry, 2020, 40(2): 454-461. doi: 10.6023/cjoc201907046.","doi":"10.6023/cjoc201907046","figContent":"yjhx-40-2-454-S1.jpg$$yjhx-40-2-454-S2.jpg$$yjhx-40-2-454-1.jpg$$yjhx-40-2-454-S3.jpg","figList":["yjhx-40-2-454-S1.jpg","yjhx-40-2-454-S2.jpg","yjhx-40-2-454-1.jpg","yjhx-40-2-454-S3.jpg"],"firstFig":"yjhx-40-2-454-S1.jpg","fpage":"454","highCitedState":"","htmlCount":433,"htmlFile":"","id":"3b4cb520-400c-420f-b85d-fe95b547ac36","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"高价碘, 8-氨基喹啉, 亲核氟化, 氟化银","keywordCn":"高价碘, 8-氨基喹啉, 亲核氟化, 氟化银","keywordCnList":["高价碘"," 8-氨基喹啉"," 亲核氟化"," 氟化银"],"keywordEn":"hypervalent iodine, 8-aminoqunoline, nucleophilic fluorination, silver fluoride","keywordEnList":["hypervalent iodine"," 8-aminoqunoline"," nucleophilic fluorination"," silver fluoride"],"keywordList":["高价碘"," 8-氨基喹啉"," 亲核氟化"," 氟化银"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"461","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":15,"pdfSize":539.15,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"高价碘试剂介导的8-氨基喹啉C(5)位碳-氢键亲核氟化反应","titleCn":"高价碘试剂介导的8-氨基喹啉C(5)位碳-氢键亲核氟化反应","titleEn":"Hypervalent Iodine Reagent-Mediated C(5) C-H Nucleophilic Fluorination of 8-Aminoqunolines","viewCount":2788,"volume":"40","year":2020},{"abstractInfo":"描述了通过钯催化2-炔基芳基叠氮一锅法氧化/水解制备2-苯甲酰胺基苯甲酸的合成方法.在温和的反应条件下，反应以良好至极好的产率完成.","abstractInfoCn":"描述了通过钯催化2-炔基芳基叠氮一锅法氧化/水解制备2-苯甲酰胺基苯甲酸的合成方法.在温和的反应条件下，反应以良好至极好的产率完成.","abstractInfoEn":"A synthetic method to prepare 2-benzoylaminobenzoic acids via Pd-catalyzed one-pot oxidation/hydrolysis from 2-alkynyl arylazides is described. The reaction was accomplished in good to excellent yields under mild reaction conditions.","articleNo":"","authorCnList":["圣戎"," 李萍"," 周志强"," 胡贵文"," 张小祥"],"authorEnList":["Sheng Rong"," Li Ping"," Zhou Zhiqiang"," Hu Guiwen"," Zhang Xiaoxiang"],"authorList":["圣戎"," 李萍"," 周志强"," 胡贵文"," 张小祥"],"authors":"圣戎, 李萍, 周志强, 胡贵文, 张小祥","authorsCn":"圣戎, 李萍, 周志强, 胡贵文, 张小祥","authorsEn":"Sheng Rong, Li Ping, Zhou Zhiqiang, Hu Guiwen, Zhang Xiaoxiang","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"圣戎, 李萍, 周志强, 胡贵文, 张小祥. 钯催化氧化/水解2-炔基芳基叠氮一锅法合成2-苯甲酰胺基苯甲酸. 有机化学, 2020, 40(2): 462-469. doi: 10.6023/cjoc201909005.","citationCn":"圣戎, 李萍, 周志强, 胡贵文, 张小祥. 钯催化氧化/水解2-炔基芳基叠氮一锅法合成2-苯甲酰胺基苯甲酸. 有机化学, 2020, 40(2): 462-469. doi: 10.6023/cjoc201909005.","citationEn":"圣戎, 李萍, 周志强, 胡贵文, 张小祥. Pd-Catalyzed One-Pot Oxidation/Hydrolysis for the Synthesis of 2-Benzoylaminobenzoic Acids from 2-Alkynyl Arylazides. Chinese Journal of Organic Chemistry, 2020, 40(2): 462-469. doi: 10.6023/cjoc201909005.","doi":"10.6023/cjoc201909005","figContent":"yjhx-40-2-462-S1.jpg$$yjhx-40-2-462-S2.jpg$$yjhx-40-2-462-S3.jpg$$yjhx-40-2-462-S4.jpg","figList":["yjhx-40-2-462-S1.jpg","yjhx-40-2-462-S2.jpg","yjhx-40-2-462-S3.jpg","yjhx-40-2-462-S4.jpg"],"firstFig":"yjhx-40-2-462-S1.jpg","fpage":"462","highCitedState":"","htmlCount":259,"htmlFile":"","id":"735b7d36-69f4-4900-a330-841777d1f6a8","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"钯催化, 一锅化反应, 氧化, 水解, 2-苯甲酰氨基苯甲酸","keywordCn":"钯催化, 一锅化反应, 氧化, 水解, 2-苯甲酰氨基苯甲酸","keywordCnList":["钯催化"," 一锅化反应"," 氧化"," 水解"," 2-苯甲酰氨基苯甲酸"],"keywordEn":"Pd-catalyzed, one-pot reaction, oxidation, hydrolysis, 2-benzoylaminobenzoic acids","keywordEnList":["Pd-catalyzed"," one-pot reaction"," oxidation"," hydrolysis"," 2-benzoylaminobenzoic acids"],"keywordList":["钯催化"," 一锅化反应"," 氧化"," 水解"," 2-苯甲酰氨基苯甲酸"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"469","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":10,"pdfSize":583.77,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"钯催化氧化/水解2-炔基芳基叠氮一锅法合成2-苯甲酰胺基苯甲酸","titleCn":"钯催化氧化/水解2-炔基芳基叠氮一锅法合成2-苯甲酰胺基苯甲酸","titleEn":"Pd-Catalyzed One-Pot Oxidation/Hydrolysis for the Synthesis of 2-Benzoylaminobenzoic Acids from 2-Alkynyl Arylazides","viewCount":2297,"volume":"40","year":2020},{"abstractInfo":"在氮杂环卡宾（NHC）催化下，查尔酮衍生物与<i>α-<\/i>溴代烯醛经过\"Michael加成-Michael加成-内酯化\"等串联过程，一步合成了官能化萘并吡喃酮.该方法具有产率高、底物易得和条件温和等优点，为萘并吡喃酮的高效构建和官能化提供了新思路.","abstractInfoCn":"在氮杂环卡宾（NHC）催化下，查尔酮衍生物与<i>α-<\/i>溴代烯醛经过\"Michael加成-Michael加成-内酯化\"等串联过程，一步合成了官能化萘并吡喃酮.该方法具有产率高、底物易得和条件温和等优点，为萘并吡喃酮的高效构建和官能化提供了新思路.","abstractInfoEn":"An efficient <i>N<\/i>-heterocyclic carbene (NHC)-catalyzed \"Michael-Michael-Lactonization\" cascade process involving chalcone derivatives and <i>α-<\/i>bromoenals for the syntheses of functionalized naphthopyranones was disclosed. This approach was qualified with good yields, readily available starting materials and mild reaction conditions.","articleNo":"","authorCnList":["李莎"," 徐嘉煜"," 罗鲜"," 杨雯涵"," 姚昌盛"],"authorEnList":["Li Sha"," Xu Jiayu"," Luo Xian"," Yang Wenhan"," Yao Changsheng"],"authorList":["李莎"," 徐嘉煜"," 罗鲜"," 杨雯涵"," 姚昌盛"],"authors":"李莎, 徐嘉煜, 罗鲜, 杨雯涵, 姚昌盛","authorsCn":"李莎, 徐嘉煜, 罗鲜, 杨雯涵, 姚昌盛","authorsEn":"Li Sha, Xu Jiayu, Luo Xian, Yang Wenhan, Yao Changsheng","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"李莎, 徐嘉煜, 罗鲜, 杨雯涵, 姚昌盛. 氮杂环卡宾催化下官能化萘并吡喃酮的串联合成. 有机化学, 2020, 40(2): 470-477. doi: 10.6023/cjoc201905034.","citationCn":"李莎, 徐嘉煜, 罗鲜, 杨雯涵, 姚昌盛. 氮杂环卡宾催化下官能化萘并吡喃酮的串联合成. 有机化学, 2020, 40(2): 470-477. doi: 10.6023/cjoc201905034.","citationEn":"李莎, 徐嘉煜, 罗鲜, 杨雯涵, 姚昌盛. Efficient <i>N<\/i>-Heterocyclic Carbene-Catalyzed Cascade Synthesis of Functionalized Naphthopyranone. Chinese Journal of Organic Chemistry, 2020, 40(2): 470-477. doi: 10.6023/cjoc201905034.","doi":"10.6023/cjoc201905034","figContent":"yjhx-40-2-470-1.jpg$$yjhx-40-2-470-S1.jpg$$yjhx-40-2-470-S2.jpg$$yjhx-40-2-470-S3.jpg$$yjhx-40-2-470-2.jpg","figList":["yjhx-40-2-470-1.jpg","yjhx-40-2-470-S1.jpg","yjhx-40-2-470-S2.jpg","yjhx-40-2-470-S3.jpg","yjhx-40-2-470-2.jpg"],"firstFig":"yjhx-40-2-470-1.jpg","fpage":"470","highCitedState":"","htmlCount":285,"htmlFile":"","id":"e1d3674d-eab4-430a-b197-3e793da62f71","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"氮杂环卡宾(NHC), <i>α-<\/i>溴代烯醛, 查尔酮衍生物, 官能化萘并吡喃酮, 串联反应","keywordCn":"氮杂环卡宾(NHC), <i>α-<\/i>溴代烯醛, 查尔酮衍生物, 官能化萘并吡喃酮, 串联反应","keywordCnList":["氮杂环卡宾(NHC)"," <i>α-<\/i>溴代烯醛"," 查尔酮衍生物"," 官能化萘并吡喃酮"," 串联反应"],"keywordEn":"<i>N<\/i>-heterocyclic carbene (NHC), <i>α-<\/i>bromoenals, chalcone derivatives, functionalized naphthopyranone, cascade reaction","keywordEnList":["<i>N<\/i>-heterocyclic carbene (NHC)"," <i>α-<\/i>bromoenals"," chalcone derivatives"," functionalized naphthopyranone"," cascade reaction"],"keywordList":["氮杂环卡宾(NHC)"," <i>α-<\/i>溴代烯醛"," 查尔酮衍生物"," 官能化萘并吡喃酮"," 串联反应"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"477","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":34,"pdfSize":1738.61,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"氮杂环卡宾催化下官能化萘并吡喃酮的串联合成","titleCn":"氮杂环卡宾催化下官能化萘并吡喃酮的串联合成","titleEn":"Efficient <i>N<\/i>-Heterocyclic Carbene-Catalyzed Cascade Synthesis of Functionalized Naphthopyranone","viewCount":2398,"volume":"40","year":2020},{"abstractInfo":"合成出了一系列新型基于咔唑的单-/双-碳酰腙衍生物<b>3<\/b>和<b>4<\/b>.利用<sup>1<\/sup>HNMR、<sup>13<\/sup>CNMR、IR和元素分析对其进行了结构表征.评价了目标化合物对蛋白酪氨酸磷酸酶1B（PTP1B）的抑制活性，讨论了结构与活性的关系.实验结果显示，大部分化合物对PTP1B具有良好的抑制活性，其中1，5-双[（9-丁基-3-咔唑基）亚甲基]碳酰腙（<b>4c<\/b>）的抑制活性最高，IC<sub>50<\/sub>=（4.81±0.41）μmol/L，且活性高于对照药物齐墩果酸.对目标化合物1-[（9-庚基-3-咔唑基）亚甲基]碳酰腙（<b>3f<\/b>）和<b>4c<\/b>进行分子对接研究和密度泛函理论（DFT）计算.分子对接结果表明，化合物<b>3f<\/b>和<b>4c<\/b>结合到PTP1B酶由螺旋α3和α6形成的活性位点，与PTP1B酶通过氢键、极性、疏水和π-π等相互作用形成了稳定的复合物.","abstractInfoCn":"合成出了一系列新型基于咔唑的单-/双-碳酰腙衍生物<b>3<\/b>和<b>4<\/b>.利用<sup>1<\/sup>H NMR、<sup>13<\/sup>C NMR、IR和元素分析对其进行了结构表征.评价了目标化合物对蛋白酪氨酸磷酸酶1B（PTP1B）的抑制活性，讨论了结构与活性的关系.实验结果显示，大部分化合物对PTP1B具有良好的抑制活性，其中1，5-双[（9-丁基-3-咔唑基）亚甲基]碳酰腙（<b>4c<\/b>）的抑制活性最高，IC<sub>50<\/sub>=（4.81±0.41）μmol/L，且活性高于对照药物齐墩果酸.对目标化合物1-[（9-庚基-3-咔唑基）亚甲基]碳酰腙（<b>3f<\/b>）和<b>4c<\/b>进行分子对接研究和密度泛函理论（DFT）计算.分子对接结果表明，化合物<b>3f<\/b>和<b>4c<\/b>结合到PTP1B酶由螺旋α3和α6形成的活性位点，与PTP1B酶通过氢键、极性、疏水和π-π等相互作用形成了稳定的复合物.","abstractInfoEn":"A series of novel carbazole-based mono-/bis-carbohydrazone derivatives <b>3<\/b> and <b>4<\/b> were synthesized. Their structures were characterized by <sup>1<\/sup>H NMR, <sup>13<\/sup>C NMR, IR spectra and elemental analysis. The inhibitory activities of all synthesized compounds against protein tyrosine phosphatase 1B (PTP1B) were evaluated, and the structure-activity relationship was discussed. The results indicated that most of the compounds had good inhibitory activity against PTP1B, and 1, 5-bis[(9-butyl-3-carba-zolyl)methylene]carbohydrazone (<b>4c<\/b>) showed the highest inhibitory activity against PTP1B with IC<sub>50<\/sub>=(4.81±0.41) μmol/L and the activity was higher than that of the control drug oleanolic acid. Molecular docking and density functional theory (DFT) calculations of <b>3f<\/b> and <b>4c<\/b> were carried out. The results of molecular docking indicated that 1-[(9-heptyl-3-carbazolyl)meth-ylene]carbohydrazone (<b>3f<\/b>) and <b>4c<\/b> bind to an active site of PTP1B enzyme formed by the helices α3 and α6, and formed a stable complex respectively with PTP1B enzyme by hydrogen bonds, polar, hydrophobic and π-π interactions.","articleNo":"","authorCnList":["李英俊"," 刘雪洁"," 刘季红"," 高立信"," 靳焜"," 盛丽"," 杨鸿境"," 林乐弟"," 李佳"],"authorEnList":["Li Yingjun"," Liu Xuejie"," Liu Jihong"," Gao Lixin"," Jin Kun"," Sheng Li"," Yang Hongjing"," Lin Ledi"," Li Jia"],"authorList":["李英俊"," 刘雪洁"," 刘季红"," 高立信"," 靳焜"," 盛丽"," 杨鸿境"," 林乐弟"," 李佳"],"authors":"李英俊, 刘雪洁, 刘季红, 高立信, 靳焜, 盛丽, 杨鸿境, 林乐弟, 李佳","authorsCn":"李英俊, 刘雪洁, 刘季红, 高立信, 靳焜, 盛丽, 杨鸿境, 林乐弟, 李佳","authorsEn":"Li Yingjun, Liu Xuejie, Liu Jihong, Gao Lixin, Jin Kun, Sheng Li, Yang Hongjing, Lin Ledi, Li Jia","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"李英俊, 刘雪洁, 刘季红, 高立信, 靳焜, 盛丽, 杨鸿境, 林乐弟, 李佳. 基于咔唑的新型碳酰腙衍生物的合成及蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性评价. 有机化学, 2020, 40(2): 478-488. doi: 10.6023/cjoc201907043.","citationCn":"李英俊, 刘雪洁, 刘季红, 高立信, 靳焜, 盛丽, 杨鸿境, 林乐弟, 李佳. 基于咔唑的新型碳酰腙衍生物的合成及蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性评价. 有机化学, 2020, 40(2): 478-488. doi: 10.6023/cjoc201907043.","citationEn":"李英俊, 刘雪洁, 刘季红, 高立信, 靳焜, 盛丽, 杨鸿境, 林乐弟, 李佳. Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Carbazole-Based Carbohydrazone Derivatives. Chinese Journal of Organic Chemistry, 2020, 40(2): 478-488. doi: 10.6023/cjoc201907043.","doi":"10.6023/cjoc201907043","figContent":"yjhx-40-2-478-S1.jpg$$yjhx-40-2-478-S2.jpg$$yjhx-40-2-478-S3.jpg$$yjhx-40-2-478-S4.jpg$$yjhx-40-2-478-1.jpg$$yjhx-40-2-478-2.jpg$$yjhx-40-2-478-3.jpg$$yjhx-40-2-478-4.jpg$$yjhx-40-2-478-5.jpg$$yjhx-40-2-478-6.jpg","figList":["yjhx-40-2-478-S1.jpg","yjhx-40-2-478-S2.jpg","yjhx-40-2-478-S3.jpg","yjhx-40-2-478-S4.jpg","yjhx-40-2-478-1.jpg","yjhx-40-2-478-2.jpg","yjhx-40-2-478-3.jpg","yjhx-40-2-478-4.jpg","yjhx-40-2-478-5.jpg","yjhx-40-2-478-6.jpg"],"firstFig":"yjhx-40-2-478-S1.jpg","fpage":"478","highCitedState":"","htmlCount":266,"htmlFile":"","id":"a449cbbc-1fe0-4a85-83d9-442e3d607c53","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"碳酰腙, 咔唑, 合成, PTP1B抑制剂, 分子对接, DFT计算","keywordCn":"碳酰腙, 咔唑, 合成, PTP1B抑制剂, 分子对接, DFT计算","keywordCnList":["碳酰腙"," 咔唑"," 合成"," PTP1B抑制剂"," 分子对接"," DFT计算"],"keywordEn":"carbohydrazone, carbazole, synthesis, PTP1B inhibitor, molecular docking, DFT calculations","keywordEnList":["carbohydrazone"," carbazole"," synthesis"," PTP1B inhibitor"," molecular docking"," DFT calculations"],"keywordList":["碳酰腙"," 咔唑"," 合成"," PTP1B抑制剂"," 分子对接"," DFT计算"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"488","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":13,"pdfSize":681.04,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"基于咔唑的新型碳酰腙衍生物的合成及蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性评价","titleCn":"基于咔唑的新型碳酰腙衍生物的合成及蛋白酪氨酸磷酸酶1B(PTP1B)抑制活性评价","titleEn":"Synthesis and Protein Tyrosine Phosphatase 1B (PTP1B) Inhibitory Activity Evaluation of Novel Carbazole-Based Carbohydrazone Derivatives","viewCount":2515,"volume":"40","year":2020},{"abstractInfo":"基于咔唑的强给电子能力合成了一种对空气稳定的齿形钯配合物催化剂（<b>C1<\/b>~<b>C6<\/b>）.这种钯催化剂可高效催化唑类和溴代芳烃的直接芳基化反应，在空气条件下，碳酸钾为碱，无需其他添加剂，即取得了较好的催化活性与底物普适性.在相对温和的条件和催化剂用量为0.5mol%时，即可实现噻唑与溴代芳烃直接芳基化反应顺利进行.值得一提的是，这是目前以KOAc为碱的反应体系中，反应活性最高的催化体系.","abstractInfoCn":"基于咔唑的强给电子能力合成了一种对空气稳定的齿形钯配合物催化剂（<b>C1<\/b>~<b>C6<\/b>）.这种钯催化剂可高效催化唑类和溴代芳烃的直接芳基化反应，在空气条件下，碳酸钾为碱，无需其他添加剂，即取得了较好的催化活性与底物普适性.在相对温和的条件和催化剂用量为0.5 mol%时，即可实现噻唑与溴代芳烃直接芳基化反应顺利进行.值得一提的是，这是目前以KOAc为碱的反应体系中，反应活性最高的催化体系.","abstractInfoEn":"A new type of pincer palladium complexes <b>C1<\/b>~C<b>6<\/b> based on the strong donor strength of carbazoles skeleton were synthesized. The air-and moisture-stable complexes <b>C1<\/b>~C<b>6<\/b> act as efficient catalysts for the direct arylation of azoles with (hetero)aryl bromides in good to excellent yields with broad substrate scope used KOAc as sole base under aerobic conditions. It was demonstrated that this developed protocol was the most catalytic system for the direct C-H bond arylation for thiazoles under relatively mild reaction conditions at a low catalyst loading of 0.5 mol%.","articleNo":"","authorCnList":["宋文越"," 饶小峰"," 卜庆青"," 刘宁"],"authorEnList":["Song Wen-Yue"," Rao Xiaofeng"," Bu Qingqing"," Liu Ning"],"authorList":["宋文越"," 饶小峰"," 卜庆青"," 刘宁"],"authors":"宋文越, 饶小峰, 卜庆青, 刘宁","authorsCn":"宋文越, 饶小峰, 卜庆青, 刘宁","authorsEn":"Song Wen-Yue, Rao Xiaofeng, Bu Qingqing, Liu Ning","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"宋文越, 饶小峰, 卜庆青, 刘宁. 咔唑桥连NCN齿形钯配合物催化的唑类C-H键直接芳基化反应. 有机化学, 2020, 40(2): 489-500. doi: 10.6023/cjoc201907035.","citationCn":"宋文越, 饶小峰, 卜庆青, 刘宁. 咔唑桥连NCN齿形钯配合物催化的唑类C-H键直接芳基化反应. 有机化学, 2020, 40(2): 489-500. doi: 10.6023/cjoc201907035.","citationEn":"宋文越, 饶小峰, 卜庆青, 刘宁. Carbazole-Bridged NCN-Pincer Palladium Complex Catalyzed Direct C-H Arylation Reaction of Azoles. Chinese Journal of Organic Chemistry, 2020, 40(2): 489-500. doi: 10.6023/cjoc201907035.","doi":"10.6023/cjoc201907035","figContent":"yjhx-40-2-489-S1.jpg$$yjhx-40-2-489-1.jpg$$yjhx-40-2-489-S2.jpg","figList":["yjhx-40-2-489-S1.jpg","yjhx-40-2-489-1.jpg","yjhx-40-2-489-S2.jpg"],"firstFig":"yjhx-40-2-489-S1.jpg","fpage":"489","highCitedState":"","htmlCount":222,"htmlFile":"","id":"7813cfee-2e32-4d73-b3b2-472e308ed10e","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"咔唑配体, 钯配合物, 直接芳基化反应, 溴代芳烃, 偶联反应","keywordCn":"咔唑配体, 钯配合物, 直接芳基化反应, 溴代芳烃, 偶联反应","keywordCnList":["咔唑配体"," 钯配合物"," 直接芳基化反应"," 溴代芳烃"," 偶联反应"],"keywordEn":"carbazole ligand, palladium complex, direct arylation, aryl bromides, coupling reaction","keywordEnList":["carbazole ligand"," palladium complex"," direct arylation"," aryl bromides"," coupling reaction"],"keywordList":["咔唑配体"," 钯配合物"," 直接芳基化反应"," 溴代芳烃"," 偶联反应"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"500","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":12,"pdfSize":1726.01,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"咔唑桥连NCN齿形钯配合物催化的唑类C-H键直接芳基化反应","titleCn":"咔唑桥连NCN齿形钯配合物催化的唑类C-H键直接芳基化反应","titleEn":"Carbazole-Bridged NCN-Pincer Palladium Complex Catalyzed Direct C-H Arylation Reaction of Azoles","viewCount":2222,"volume":"40","year":2020},{"abstractInfo":"在酸催化及脱水作用下，以2-（4-二丁基氨基-2-羟基苯甲酰基）苯甲酸或2-（4-二乙基氨基-2-羟基苯甲酰基）苯甲酸和吡唑啉酮为原料，通过Knoevenagel缩合和脱水反应，合成了一系列新型螺[色烯并（2，3<i>-c<\/i>）吡唑-4，1'-异苯并呋喃]-3'-酮类化合物.考察了反应物配比、催化剂、温度和时间等因素对反应的影响，初步探究了所合成化合物在不同pH、溶剂中的光学性能，其中1-（4-氯苯基）-7-（二乙基氨基）-3-甲基-1<i>H<\/i>，3'<i>H<\/i>-螺[色烯并[2，3-<i>c<\/i>]吡唑-4，1'-异苯并呋喃]-3'-酮（<b>1e<\/b>）和1-（4-氯苯基）-7-（二丁基氨基）-3-甲基-1<i>H<\/i>，3'<i>H<\/i>-螺[色烯并[2，3-<i>c<\/i>]吡唑-4，1'-异苯并呋喃]-3'-酮（<b>1j<\/b>）有潜力作为强酸强碱的pH指示剂.","abstractInfoCn":"在酸催化及脱水作用下，以2-（4-二丁基氨基-2-羟基苯甲酰基）苯甲酸或2-（4-二乙基氨基-2-羟基苯甲酰基）苯甲酸和吡唑啉酮为原料，通过Knoevenagel缩合和脱水反应，合成了一系列新型螺[色烯并（2，3<i>-c<\/i>）吡唑-4，1'-异苯并呋喃]-3'-酮类化合物.考察了反应物配比、催化剂、温度和时间等因素对反应的影响，初步探究了所合成化合物在不同pH、溶剂中的光学性能，其中1-（4-氯苯基）-7-（二乙基氨基）-3-甲基-1<i>H<\/i>，3'<i>H<\/i>-螺[色烯并[2，3-<i>c<\/i>]吡唑-4，1'-异苯并呋喃]-3'-酮（<b>1e<\/b>）和1-（4-氯苯基）-7-（二丁基氨基）-3-甲基-1<i>H<\/i>，3'<i>H<\/i>-螺[色烯并[2，3-<i>c<\/i>]吡唑-4，1'-异苯并呋喃]-3'-酮（<b>1j<\/b>）有潜力作为强酸强碱的pH指示剂.","abstractInfoEn":"A series of novel spiro[chromo(2, 3-<i>c<\/i>)pyrazole-4, 1'-isobenzofuran]-3'-one compounds were synthesized via Knoevenagel condensation and dehydration reaction of 2-(4-dibutylamino-2-hydroxybenzoyl)benzoic acid or 2-[4-(diethylamino)-2-hydroxybenzoyl]benzoic acid with pyrazolones using acid as catalysts and dehydrants. The effects of the ratio of the substrates, catalyst, temperature and reaction time were examined. Their optical properties in different pH and solvent were investigated. It shows that 1-(4-chlorophenyl)-7-(diethylamino)-3-methyl-1<i>H<\/i>, 3'<i>H<\/i>-spiro[chromene[2, 3-<i>c<\/i>]pyrazole-4, 1'-isobenzofuran]-3'-one (<b>1e<\/b>) and 1-(4-chlorophenyl)-7-(dibutylamino)-3-methyl-1<i>H<\/i>, 3'<i>H<\/i>-spiro[chromene[2, 3-<i>c<\/i>]pyrazole-4, 1'-isobenzofuran]-3'-one (<b>1j<\/b>) have potential as pH indicators for strong acids and bases.","articleNo":"","authorCnList":["岳永双"," 解正峰"," 褚义成"," 薛松松"],"authorEnList":["Yue Yongshuang"," Xie Zhengfeng"," Chu Yicheng"," Xue Songsong"],"authorList":["岳永双"," 解正峰"," 褚义成"," 薛松松"],"authors":"岳永双, 解正峰, 褚义成, 薛松松","authorsCn":"岳永双, 解正峰, 褚义成, 薛松松","authorsEn":"Yue Yongshuang, Xie Zhengfeng, Chu Yicheng, Xue Songsong","categoryName":"研究论文","categoryNameCn":"研究论文","categoryNameEn":"Articles","citation":"岳永双, 解正峰, 褚义成, 薛松松. 新型螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮类化合物的合成及光学性能研究. 有机化学, 2020, 40(2): 501-510. doi: 10.6023/cjoc201907033.","citationCn":"岳永双, 解正峰, 褚义成, 薛松松. 新型螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮类化合物的合成及光学性能研究. 有机化学, 2020, 40(2): 501-510. doi: 10.6023/cjoc201907033.","citationEn":"岳永双, 解正峰, 褚义成, 薛松松. Synthesis and Optical Properties of Novel Spiro[chromo(2, 3-<i>c<\/i>)-pyrazole-4, 1'-isobenzofuran]-3'-one Compounds. Chinese Journal of Organic Chemistry, 2020, 40(2): 501-510. doi: 10.6023/cjoc201907033.","doi":"10.6023/cjoc201907033","figContent":"yjhx-40-2-501-1.jpg$$yjhx-40-2-501-2.jpg$$yjhx-40-2-501-3.jpg$$yjhx-40-2-501-4.jpg$$yjhx-40-2-501-5.jpg$$yjhx-40-2-501-S1.jpg$$yjhx-40-2-501-6.jpg$$yjhx-40-2-501-7.jpg","figList":["yjhx-40-2-501-1.jpg","yjhx-40-2-501-2.jpg","yjhx-40-2-501-3.jpg","yjhx-40-2-501-4.jpg","yjhx-40-2-501-5.jpg","yjhx-40-2-501-S1.jpg","yjhx-40-2-501-6.jpg","yjhx-40-2-501-7.jpg"],"firstFig":"yjhx-40-2-501-1.jpg","fpage":"501","highCitedState":"","htmlCount":479,"htmlFile":"","id":"7172c4ec-16e3-496f-a9c8-5460ee018ae6","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮, 吡唑啉酮, Knoevenagel反应, pH","keywordCn":"螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮, 吡唑啉酮, Knoevenagel反应, pH","keywordCnList":["螺[色烯并(2"," 3-<i>c<\/i>)吡唑-4"," 1'-异苯并呋喃]-3'-酮"," 吡唑啉酮"," Knoevenagel反应"," pH"],"keywordEn":"spiro[chromo(2, 3-<i>c<\/i>)pyrazole-4, 1'-isobenzofuran]-3'-one, pyrazolone, Knoevenagel reaction, pH","keywordEnList":["spiro[chromo(2"," 3-<i>c<\/i>)pyrazole-4"," 1'-isobenzofuran]-3'-one"," pyrazolone"," Knoevenagel reaction"," pH"],"keywordList":["螺[色烯并(2"," 3-<i>c<\/i>)吡唑-4"," 1'-异苯并呋喃]-3'-酮"," 吡唑啉酮"," Knoevenagel反应"," pH"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"510","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":10,"pdfSize":1186.55,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"新型螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮类化合物的合成及光学性能研究","titleCn":"新型螺[色烯并(2, 3-<i>c<\/i>)吡唑-4, 1'-异苯并呋喃]-3'-酮类化合物的合成及光学性能研究","titleEn":"Synthesis and Optical Properties of Novel Spiro[chromo(2, 3-<i>c<\/i>)-pyrazole-4, 1'-isobenzofuran]-3'-one Compounds","viewCount":2747,"volume":"40","year":2020}],"研究简报":[{"abstractInfo":"过氧亚硝酸根（ONOO<sup>-<\/sup>）是生物体内的一种重要的活性氧，与人体内的各种生理活动息息相关.利用苯并吡喃腈-香豆素体系，合成了一种用于ONOO<sup>-<\/sup>检测的近红外比率型荧光探针（<i>E<\/i>）-7-（二乙胺基）-3-（2-（苯并吡喃腈）乙烯基）-香豆素（<b>DCCM<\/b>）.该探针在ONOO<sup>-<\/sup>存在下表现出强烈的响应，颜色从紫色变为浅粉色，最大发射峰蓝移217nm，荧光颜色从淡紫色变为蓝色，能够直观地对溶液中的ONOO<sup>-<\/sup>进行监测.<b>DCCM<\/b>可以灵敏地检测ONOO<sup>-<\/sup>，最低检测限为6.0×10<sup>-7<\/sup>mol·L<sup>-1<\/sup>，该探针被成功用于HeLa细胞中的ONOO<sup>-<\/sup>成像检测.","abstractInfoCn":"过氧亚硝酸根（ONOO<sup>-<\/sup>）是生物体内的一种重要的活性氧，与人体内的各种生理活动息息相关.利用苯并吡喃腈-香豆素体系，合成了一种用于ONOO<sup>-<\/sup>检测的近红外比率型荧光探针（<i>E<\/i>）-7-（二乙胺基）-3-（2-（苯并吡喃腈）乙烯基）-香豆素（<b>DCCM<\/b>）.该探针在ONOO<sup>-<\/sup>存在下表现出强烈的响应，颜色从紫色变为浅粉色，最大发射峰蓝移217 nm，荧光颜色从淡紫色变为蓝色，能够直观地对溶液中的ONOO<sup>-<\/sup>进行监测.<b>DCCM<\/b>可以灵敏地检测ONOO<sup>-<\/sup>，最低检测限为6.0×10<sup>-7<\/sup> mol·L<sup>-1<\/sup>，该探针被成功用于HeLa细胞中的ONOO<sup>-<\/sup>成像检测.","abstractInfoEn":"Peroxynitrite (ONOO<sup>-<\/sup>) is an important reactive oxygen species in living organisms, and is associated with various biological process in human body. Using dicyanomethylene-4<i>H<\/i>-pyran coumarin system, a near-infrared ratiometric fluorescent probe (<i>E<\/i>)-7-(diethylamino)-3-(2-(dicyanomethylene-4<i>H<\/i>-pyran)vinyl)-coumarin (<b>DCCM<\/b>) was developed for ONOO<sup>-<\/sup> detec-tion. This probe exhibited a strong response in the presence of ONOO<sup>-<\/sup>, with a significant color change from purple to light pink, along with 217 nm fluorescence blue shift. The emission color changed from heliotrope to blue, which enables the monitoring of ONOO<sup>-<\/sup> by naked eyes. <b>DCCM<\/b> was used to sensitively measure ONOO<sup>-<\/sup> with low detection limit of 6.0×10<sup>-7<\/sup> mol·L<sup>-1<\/sup>. The use of <b>DCCM<\/b> for imaging ONOO<sup>-<\/sup> in HeLa cells was also demonstrated.","articleNo":"","authorCnList":["陈宇"," 毕克英"," 郝瑞亭"," 谢萍"," 黄丽娜"," 王玉敏"," 张俊峰"," 徐锐"," 吴相华"],"authorEnList":["Chen Yu"," Bi Keying"," Hao Ruiting"," Xie Ping"," Huang Lina"," Wang Yumin"," Zhang Junfeng"," Xu Rui"," Wu Xianghua"],"authorList":["陈宇"," 毕克英"," 郝瑞亭"," 谢萍"," 黄丽娜"," 王玉敏"," 张俊峰"," 徐锐"," 吴相华"],"authors":"陈宇, 毕克英, 郝瑞亭, 谢萍, 黄丽娜, 王玉敏, 张俊峰, 徐锐, 吴相华","authorsCn":"陈宇, 毕克英, 郝瑞亭, 谢萍, 黄丽娜, 王玉敏, 张俊峰, 徐锐, 吴相华","authorsEn":"Chen Yu, Bi Keying, Hao Ruiting, Xie Ping, Huang Lina, Wang Yumin, Zhang Junfeng, Xu Rui, Wu Xianghua","categoryName":"研究简报","categoryNameCn":"研究简报","categoryNameEn":"Notes","citation":"陈宇, 毕克英, 郝瑞亭, 谢萍, 黄丽娜, 王玉敏, 张俊峰, 徐锐, 吴相华. 基于苯并吡喃腈-香豆素体系的近红外比率型荧光探针用于检测HeLa细胞中的过氧亚硝酸盐. 有机化学, 2020, 40(2): 511-515. doi: 10.6023/cjoc201907048.","citationCn":"陈宇, 毕克英, 郝瑞亭, 谢萍, 黄丽娜, 王玉敏, 张俊峰, 徐锐, 吴相华. 基于苯并吡喃腈-香豆素体系的近红外比率型荧光探针用于检测HeLa细胞中的过氧亚硝酸盐. 有机化学, 2020, 40(2): 511-515. doi: 10.6023/cjoc201907048.","citationEn":"陈宇, 毕克英, 郝瑞亭, 谢萍, 黄丽娜, 王玉敏, 张俊峰, 徐锐, 吴相华. Near-Infrared Ratiometric Fluorescent Probe for Detection of Peroxynitrite in HeLa Cells Based on Dicyanomethylene-4<i>H<\/i>-pyran Coumarin System. Chinese Journal of Organic Chemistry, 2020, 40(2): 511-515. doi: 10.6023/cjoc201907048.","doi":"10.6023/cjoc201907048","figContent":"yjhx-40-2-511-S1.jpg$$yjhx-40-2-511-1.jpg$$yjhx-40-2-511-2.jpg$$yjhx-40-2-511-S2.jpg$$yjhx-40-2-511-3.jpg$$yjhx-40-2-511-4.jpg","figList":["yjhx-40-2-511-S1.jpg","yjhx-40-2-511-1.jpg","yjhx-40-2-511-2.jpg","yjhx-40-2-511-S2.jpg","yjhx-40-2-511-3.jpg","yjhx-40-2-511-4.jpg"],"firstFig":"yjhx-40-2-511-S1.jpg","fpage":"511","highCitedState":"","htmlCount":349,"htmlFile":"","id":"20d9347f-3a82-4079-b5d8-14575ac4b9c0","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"荧光探针, 比率探针, 过氧亚硝酸盐, 细胞成像","keywordCn":"荧光探针, 比率探针, 过氧亚硝酸盐, 细胞成像","keywordCnList":["荧光探针"," 比率探针"," 过氧亚硝酸盐"," 细胞成像"],"keywordEn":"fluorescence probe, ratiometric probe, peroxynitrite, cell imaging","keywordEnList":["fluorescence probe"," ratiometric probe"," peroxynitrite"," cell imaging"],"keywordList":["荧光探针"," 比率探针"," 过氧亚硝酸盐"," 细胞成像"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"515","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":20,"pdfSize":560.31,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"基于苯并吡喃腈-香豆素体系的近红外比率型荧光探针用于检测HeLa细胞中的过氧亚硝酸盐","titleCn":"基于苯并吡喃腈-香豆素体系的近红外比率型荧光探针用于检测HeLa细胞中的过氧亚硝酸盐","titleEn":"Near-Infrared Ratiometric Fluorescent Probe for Detection of Peroxynitrite in HeLa Cells Based on Dicyanomethylene-4<i>H<\/i>-pyran Coumarin System","viewCount":2577,"volume":"40","year":2020},{"abstractInfo":"耐格霉素是具有抗革兰氏阴性菌活性的天然产物.以廉价易得的3-羰基-4-氯丁酸乙酯为原料，以八步29%的总收率实现了耐格霉素的形式合成.该工作改进了文献的合成路线，利用生物催化不对称还原高立体选择性引入C-5位的手性羟基，并将危险的叠氮引入反应放在合成后期，降低合成路线的操作风险.分子中C-3位的仲碳胺基手性中心通过Ellamn试剂介导的不对称Mannich反应构建.该路线易于放大，有望为构建耐格霉素类似物分子库以及高通量药物筛选奠定基础.","abstractInfoCn":"耐格霉素是具有抗革兰氏阴性菌活性的天然产物.以廉价易得的3-羰基-4-氯丁酸乙酯为原料，以八步29%的总收率实现了耐格霉素的形式合成.该工作改进了文献的合成路线，利用生物催化不对称还原高立体选择性引入C-5位的手性羟基，并将危险的叠氮引入反应放在合成后期，降低合成路线的操作风险.分子中C-3位的仲碳胺基手性中心通过Ellamn试剂介导的不对称Mannich反应构建.该路线易于放大，有望为构建耐格霉素类似物分子库以及高通量药物筛选奠定基础.","abstractInfoEn":"Negamycin is a potent gram-negative antibiotic. By using commercial available ethyl 4-chlorobutyrate as starting material, the formal synthesis of negamycin was achieved within 8 steps and 29% overall yield. This modified synthetic route features <i>in-situ<\/i> enzymatic promoted asmmetric reduction reaction to introduce chiral hydroxy group at C-5, a late-stage azidination at C-6 to avoid the introduction of explosive azide group in the early stage in previous syntheses. The C-3 aza-chiral center was constructed via Ellman reagent-based asymmetric Mannich reaction. This efficient route is scalable and suitable to establish a library of negamycin analogues for future high-throughput screening.","articleNo":"","authorCnList":["张世举"," 李晓彤"," 王燕"," 郑宇璁"," 韩世清"," 郁惠蕾"," 黄莎华"],"authorEnList":["Zhang Shiju"," Li Xiaotong"," Wang Yan"," Zheng Yucong"," Han Shiqing"," Yu Huilei"," Huang Shahua"],"authorList":["张世举"," 李晓彤"," 王燕"," 郑宇璁"," 韩世清"," 郁惠蕾"," 黄莎华"],"authors":"张世举, 李晓彤, 王燕, 郑宇璁, 韩世清, 郁惠蕾, 黄莎华","authorsCn":"张世举, 李晓彤, 王燕, 郑宇璁, 韩世清, 郁惠蕾, 黄莎华","authorsEn":"Zhang Shiju, Li Xiaotong, Wang Yan, Zheng Yucong, Han Shiqing, Yu Huilei, Huang Shahua","categoryName":"研究简报","categoryNameCn":"研究简报","categoryNameEn":"Note","citation":"张世举, 李晓彤, 王燕, 郑宇璁, 韩世清, 郁惠蕾, 黄莎华. 抗革兰氏阴性菌耐格霉素的形式合成. 有机化学, 2020, 40(2): 521-527. doi: 10.6023/cjoc201908025.","citationCn":"张世举, 李晓彤, 王燕, 郑宇璁, 韩世清, 郁惠蕾, 黄莎华. 抗革兰氏阴性菌耐格霉素的形式合成. 有机化学, 2020, 40(2): 521-527. doi: 10.6023/cjoc201908025.","citationEn":"张世举, 李晓彤, 王燕, 郑宇璁, 韩世清, 郁惠蕾, 黄莎华. Formal Synthesis of Gram-Negative Antibiotic Negamycin. Chinese Journal of Organic Chemistry, 2020, 40(2): 521-527. doi: 10.6023/cjoc201908025.","doi":"10.6023/cjoc201908025","figContent":"yjhx-40-2-521-1.jpg$$yjhx-40-2-521-S1.jpg$$yjhx-40-2-521-S2.jpg$$yjhx-40-2-521-S3.jpg","figList":["yjhx-40-2-521-1.jpg","yjhx-40-2-521-S1.jpg","yjhx-40-2-521-S2.jpg","yjhx-40-2-521-S3.jpg"],"firstFig":"yjhx-40-2-521-1.jpg","fpage":"521","highCitedState":"","htmlCount":383,"htmlFile":"","id":"6074fb5a-533f-42cf-9a17-4b2b13a22bdb","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"耐格霉素, Mannich反应, 革兰氏阴性菌, 形式合成","keywordCn":"耐格霉素, Mannich反应, 革兰氏阴性菌, 形式合成","keywordCnList":["耐格霉素"," Mannich反应"," 革兰氏阴性菌"," 形式合成"],"keywordEn":"negamycin, Mannich reaction, gram-negative pathogens, formal synthesis","keywordEnList":["negamycin"," Mannich reaction"," gram-negative pathogens"," formal synthesis"],"keywordList":["耐格霉素"," Mannich反应"," 革兰氏阴性菌"," 形式合成"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"527","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":20,"pdfSize":610.63,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"抗革兰氏阴性菌耐格霉素的形式合成","titleCn":"抗革兰氏阴性菌耐格霉素的形式合成","titleEn":"Formal Synthesis of Gram-Negative Antibiotic Negamycin","viewCount":2517,"volume":"40","year":2020},{"abstractInfo":"为了寻找具有生物活性的新型芳香基噻唑联哌啶酰胺类先导化合物，设计并合成了15个未见文献报道的芳基噻唑联哌啶酰胺类化合物，其结构经<sup>1<\/sup>HNMR、<sup>13<\/sup>CNMR和HRMS确证，生物活性测定结果显示，部分目标化合物表现出高效的抑菌和杀虫活性，如在200μg/mL浓度下，5-（3-溴苯基）-4-甲基-2-（1-（（4-硝基苯基）磺酰基）哌啶-4-基）噻唑（<b>6b<\/b>）对黄瓜霜霉病的抑菌活性为100%，优于嘧菌酯，5-（4-溴苯基）-2-（1-（（4-氯苯基）磺酰基）哌啶-4-基）-4-甲基噻唑（<b>6c<\/b>）对水稻纹枯病的抑菌活性为58.86%，与嘧菌酯相当；在500μg/mL浓度下，（4-（5-（3-溴苯基）-4-甲基噻唑-2-基）哌啶-1-基）（间甲基苯基）酮（<b>6h<\/b>）对粘虫的杀虫活性为100%.","abstractInfoCn":"为了寻找具有生物活性的新型芳香基噻唑联哌啶酰胺类先导化合物，设计并合成了15个未见文献报道的芳基噻唑联哌啶酰胺类化合物，其结构经<sup>1<\/sup>H NMR、<sup>13<\/sup>C NMR和HRMS确证，生物活性测定结果显示，部分目标化合物表现出高效的抑菌和杀虫活性，如在200 μg/mL浓度下，5-（3-溴苯基）-4-甲基-2-（1-（（4-硝基苯基）磺酰基）哌啶-4-基）噻唑（<b>6b<\/b>）对黄瓜霜霉病的抑菌活性为100%，优于嘧菌酯，5-（4-溴苯基）-2-（1-（（4-氯苯基）磺酰基）哌啶-4-基）-4-甲基噻唑（<b>6c<\/b>）对水稻纹枯病的抑菌活性为58.86%，与嘧菌酯相当；在500 μg/mL浓度下，（4-（5-（3-溴苯基）-4-甲基噻唑-2-基）哌啶-1-基）（间甲基苯基）酮（<b>6h<\/b>）对粘虫的杀虫活性为100%.","abstractInfoEn":"In order to find a novel biologically active compound containing aromatic thiazole piperidine structure, 15 novel aryl thiazole piperidine amide derivatives were designed and synthesized. The structures of the target compounds were fully characterized by <sup>1<\/sup>H NMR, <sup>13<\/sup>C NMR and HRMS spectra. The bioactivity test showed that some target compounds had good fungicidal and insecticidal activity. For example, the inhibition rate of 5-(3-bromophenyl)-4-methyl-2-(1-((4-nitrophenyl)-sulfonyl)piperidin-4-yl)thiazole (<b>6b<\/b>) against <i>Pseudoperonospora cubensis<\/i> was 100% better than azoxystrobin, and the inhibition rate of 5-(4-bromophenyl)-2-(1-((4-chlorophenyl)sulfonyl)piperidin-4-yl)-4-methylthiazole (<b>6c<\/b>) against <i>Rhizoctonia solani<\/i> was 58.86% comparable to azoxystrobin at 200 μg/mL. The lethal rate of (4-(5-(3-bromophenyl)-4-methylthiazol-2-yl) piperidin-1-yl) (<i>m<\/i>-tolyl)methanone (<b>6h<\/b>) against <i>Mythimna separata<\/i> was 100% at 500 μg/mL.","articleNo":"","authorCnList":["丁成荣"," 潘亚运"," 谭成侠"],"authorEnList":["Ding Chengrong"," Pan Yayun"," Tan Chengxia"],"authorList":["丁成荣"," 潘亚运"," 谭成侠"],"authors":"丁成荣, 潘亚运, 谭成侠","authorsCn":"丁成荣, 潘亚运, 谭成侠","authorsEn":"Ding Chengrong, Pan Yayun, Tan Chengxia","categoryName":"研究简报","categoryNameCn":"研究简报","categoryNameEn":"Note","citation":"丁成荣, 潘亚运, 谭成侠. 芳基噻唑联哌啶酰胺类化合物的合成及生物活性. 有机化学, 2020, 40(2): 528-535. doi: 10.6023/cjoc201907034.","citationCn":"丁成荣, 潘亚运, 谭成侠. 芳基噻唑联哌啶酰胺类化合物的合成及生物活性. 有机化学, 2020, 40(2): 528-535. doi: 10.6023/cjoc201907034.","citationEn":"丁成荣, 潘亚运, 谭成侠. Synthesis and Biological Activity of Aryl Thiazole Piperidine Amide Compounds. Chinese Journal of Organic Chemistry, 2020, 40(2): 528-535. doi: 10.6023/cjoc201907034.","doi":"10.6023/cjoc201907034","figContent":"yjhx-40-2-528-1.jpg$$yjhx-40-2-528-S1.jpg$$yjhx-40-2-528-S2.jpg$$yjhx-40-2-528-2.jpg","figList":["yjhx-40-2-528-1.jpg","yjhx-40-2-528-S1.jpg","yjhx-40-2-528-S2.jpg","yjhx-40-2-528-2.jpg"],"firstFig":"yjhx-40-2-528-1.jpg","fpage":"528","highCitedState":"","htmlCount":309,"htmlFile":"","id":"caf81b5a-e633-43d3-bced-17ae2b2d8ec5","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"噻唑联哌啶, 芳香结构, 抑菌活性, 杀虫活性","keywordCn":"噻唑联哌啶, 芳香结构, 抑菌活性, 杀虫活性","keywordCnList":["噻唑联哌啶"," 芳香结构"," 抑菌活性"," 杀虫活性"],"keywordEn":"piperidinylthiazole, aromatic structure, fungicidal activity, insecticidal activity","keywordEnList":["piperidinylthiazole"," aromatic structure"," fungicidal activity"," insecticidal activity"],"keywordList":["噻唑联哌啶"," 芳香结构"," 抑菌活性"," 杀虫活性"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"535","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":13,"pdfSize":867.21,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"芳基噻唑联哌啶酰胺类化合物的合成及生物活性","titleCn":"芳基噻唑联哌啶酰胺类化合物的合成及生物活性","titleEn":"Synthesis and Biological Activity of Aryl Thiazole Piperidine Amide Compounds","viewCount":2667,"volume":"40","year":2020},{"abstractInfo":"利用靶向策略设计了抗肿瘤药物<i>N<\/i>-（<i>N<\/i>'-苄氧羰基甘氨酰脯氨酰）丙卡巴肼（Z-GP-Pcb），发展了3步法合成丙卡巴肼（Pcb）.首先以4-甲基苯甲醛为原料，经二溴异氰脲酸（DBI）转化为<i>N<\/i>-异丙基-4-甲基苯酰胺.该化合物经2-碘酰基苯甲酸（IBX）直接氧化为<i>N<\/i>-异丙基-4-甲酰基苯酰胺，随后还原胺化得Pcb.最后与<i>N<\/i>-苄氧羰基甘氨酰脯氨酸缩合得Z-GP-Pcb，总收率49.9%.另外，本研究还建立了体外平行人造膜渗透测血脑屏障（PAMPA-BBB）方法评价Z-GP-Pcb透过血脑屏障（BBB）活性，发现其透膜常数（<i>P<\/i><sub>e<\/sub>）为（19.22±4.25）×10<sup>-6<\/sup>cm·s<sup>-1<\/sup>，大于母药Pcb[（11.14±1.34））×10<sup>-6<\/sup>cm·s<sup>-1<\/sup>]，具有较高的透过BBB活性.","abstractInfoCn":"利用靶向策略设计了抗肿瘤药物<i>N<\/i>-（<i>N<\/i>'-苄氧羰基甘氨酰脯氨酰）丙卡巴肼（Z-GP-Pcb），发展了3步法合成丙卡巴肼（Pcb）.首先以4-甲基苯甲醛为原料，经二溴异氰脲酸（DBI）转化为<i>N<\/i>-异丙基-4-甲基苯酰胺.该化合物经2-碘酰基苯甲酸（IBX）直接氧化为<i>N<\/i>-异丙基-4-甲酰基苯酰胺，随后还原胺化得Pcb.最后与<i>N<\/i>-苄氧羰基甘氨酰脯氨酸缩合得Z-GP-Pcb，总收率49.9%.另外，本研究还建立了体外平行人造膜渗透测血脑屏障（PAMPA-BBB）方法评价Z-GP-Pcb透过血脑屏障（BBB）活性，发现其透膜常数（<i>P<\/i><sub>e<\/sub>）为（19.22±4.25）×10<sup>-6<\/sup> cm·s<sup>-1<\/sup>，大于母药Pcb[（11.14±1.34））×10<sup>-6<\/sup> cm· s<sup>-1<\/sup>]，具有较高的透过BBB活性.","abstractInfoEn":"Anti-cancer drug <i>N<\/i>-(<i>N'<\/i>-carbobenzoxyglycylprolyl)procarbazine (Z-GP-Pcb) has been designed based on targeting strategy and a 3-step method has been developed for the synthesis of procarbazine (Pcb). Firstly, 4-methylbenaldehyde, as starting material, was transformed into <i>N<\/i>-isopropyl-4-methylbenzamide using dibromoisocyanuric acid (DBI). This compound was then directly oxidized to <i>N<\/i>-isopropyl-4-formylbenzamide by 2-iodoxybenzoic acid (IBX). A reductive amination reaction was then followed leading to Pcb. At last, Pcb was condensed with <i>N<\/i>-carbobenzoxyglycylproline resulting in Z-GP-Pcb. The overall yield was 49.9%. Furthermore, an <i>in vitro<\/i> blood-brain barrier (BBB) permeation assay (PAMPA-BBB) was set up to evaluate the permeation activity of Z-GP-Pcb. It was found that the permeation constant (<i>P<\/i><sub>e<\/sub>) was (19.22±4.25)×10<sup>-6<\/sup> cm·s<sup>-1<\/sup>, which was more than that of the parent drug Pcb[(11.14±1.34))×10<sup>-6<\/sup> cm·s<sup>-1<\/sup>]. This evidence suggests that Z-GP-Pcb possesses high activity to penetrate BBB.","articleNo":"","authorCnList":["张潮"," 刘志军"," 李艳冰"," 何业谱"," 林晓洪"," 陈河如"],"authorEnList":["Zhang Chao"," Liu Zhijun"," Li Yanbing"," He Yepu"," Lin Xiaohong"," Chen Heru"],"authorList":["张潮"," 刘志军"," 李艳冰"," 何业谱"," 林晓洪"," 陈河如"],"authors":"张潮, 刘志军, 李艳冰, 何业谱, 林晓洪, 陈河如","authorsCn":"张潮, 刘志军, 李艳冰, 何业谱, 林晓洪, 陈河如","authorsEn":"Zhang Chao, Liu Zhijun, Li Yanbing, He Yepu, Lin Xiaohong, Chen Heru","categoryName":"研究简报","categoryNameCn":"研究简报","categoryNameEn":"Note","citation":"张潮, 刘志军, 李艳冰, 何业谱, 林晓洪, 陈河如. 靶向抗肿瘤药<i>N<\/i>-(<i>N'<\/i>-苄氧羰基甘氨酰脯氨酰)丙卡巴肼(Z-GP-Pcb)的环境友好合成及其透过血脑屏障活性评价. 有机化学, 2020, 40(2): 536-540. doi: 10.6023/cjoc201908015.","citationCn":"张潮, 刘志军, 李艳冰, 何业谱, 林晓洪, 陈河如. 靶向抗肿瘤药<i>N<\/i>-(<i>N'<\/i>-苄氧羰基甘氨酰脯氨酰)丙卡巴肼(Z-GP-Pcb)的环境友好合成及其透过血脑屏障活性评价. 有机化学, 2020, 40(2): 536-540. doi: 10.6023/cjoc201908015.","citationEn":"张潮, 刘志军, 李艳冰, 何业谱, 林晓洪, 陈河如. Environment-Friendly Synthesis of Targeted Anticancer Drug <i>N<\/i>-(<i>N'<\/i>-Carbobenzoxyglycylprolyl)procarbazine (Z-GP-Pcb) and the Evaluation of Its Activity to Penetrate Blood-Brain Barrier. Chinese Journal of Organic Chemistry, 2020, 40(2): 536-540. doi: 10.6023/cjoc201908015.","doi":"10.6023/cjoc201908015","figContent":"yjhx-40-2-536-S1.jpg$$yjhx-40-2-536-1.jpg","figList":["yjhx-40-2-536-S1.jpg","yjhx-40-2-536-1.jpg"],"firstFig":"yjhx-40-2-536-S1.jpg","fpage":"536","highCitedState":"","htmlCount":477,"htmlFile":"","id":"c796e784-c8cb-4d7e-87ae-4199868a6d9a","issnPpub":"0253-2786","issue":"2","journalPublishId":"yjhx","journalReferenceCodeType":0,"journalTitleCn":"有机化学","journalTitleEn":"Chinese Journal of Organic Chemistry","keyword":"药物合成, 丙卡巴肼, 药物设计, 靶向抗肿瘤, 成纤维细胞激活蛋白<i>α<\/i>","keywordCn":"药物合成, 丙卡巴肼, 药物设计, 靶向抗肿瘤, 成纤维细胞激活蛋白<i>α<\/i>","keywordCnList":["药物合成"," 丙卡巴肼"," 药物设计"," 靶向抗肿瘤"," 成纤维细胞激活蛋白<i>α<\/i>"],"keywordEn":"drug synthesis, procarbazine, drug design, targeted anti-cancer, fibroblast activation protein-<i>α<\/i>","keywordEnList":["drug synthesis"," procarbazine"," drug design"," targeted anti-cancer"," fibroblast activation protein-<i>α<\/i>"],"keywordList":["药物合成"," 丙卡巴肼"," 药物设计"," 靶向抗肿瘤"," 成纤维细胞激活蛋白<i>α<\/i>"],"language":"zh","latestInfo":"","latestState":"","latestStateEn":"","lpage":"540","oldUrl":"http://sioc-journal.cn/Jwk_yjhx/CN/volumn/home.shtml","pdfDownCount":14,"pdfSize":673.48,"pubDate":"2020-02-25","recommendState":"","releaseState":"1","secCount":0,"title":"靶向抗肿瘤药<i>N<\/i>-(<i>N'<\/i>-苄氧羰基甘氨酰脯氨酰)丙卡巴肼(Z-GP-Pcb)的环境友好合成及其透过血脑屏障活性评价","titleCn":"靶向抗肿瘤药<i>N<\/i>-(<i>N'<\/i>-苄氧羰基甘氨酰脯氨酰)丙卡巴肼(Z-GP-Pcb)的环境友好合成及其透过血脑屏障活性评价","titleEn":"Environment-Friendly Synthesis of Targeted Anticancer Drug <i>N<\/i>-(<i>N'<\/i>-Carbobenzoxyglycylprolyl)procarbazine (Z-GP-Pcb) and the Evaluation of Its Activity to Penetrate Blood-Brain Barrier","viewCount":3122,"volume":"40","year":2020}],"Note":[{"abstractInfo":"Anewkindoforganicluminescentmaterialscontaininghalogen-substitutedphthalimidegroupandcarbazolesubunithavebeenconvenientlysynthesized.Theynotonlyshowedstrongaggregation-inducedemission(AIE)effect,butalsoexhibitedthermallyactivateddelayedfluorescence(TADF)infilmsandcrystallization-inducedroom-temperaturephosphorescence(RTP)properties.Especially,RTPwithmarkedafterglowfor<b>Br-AI-Cz<\/b>wasobservedbynakedeye,whichcouldbeusedasthepromisingsmartmaterialsfortheencryptionapplication.","abstractInfoCn":"方便地合成了三个含有卤素取代邻苯二甲酰亚胺与咔唑基团的新型有机发光材料<b>Br-Al-Cz<\/b>，<b>Cl-Al-Cz<\/b>和<b>F-AI-Cz<\/b>，发现它们不仅具有强的聚集诱导发光效应，而且显示膜态下热激活延迟荧光以及晶态诱导的室温磷光性质.尤其是化合物<b>Br-Al-Cz<\/b>表现出肉眼可见的长余辉室温磷光现象，因此在数据加密等中具有潜在用途.","abstractInfoEn":"A new kind of organic luminescent materials containing halogen-substituted phthalimide group and carbazole subunit have been conveniently synthesized. They not only showed strong aggregation-induced emission (AIE) effect, but also exhibited thermally activated delayed fluorescence (TADF) in films and crystallization-induced room-temperature phosphorescence (RTP) properties. Especially, RTP with marked afterglow for <b>Br-AI-Cz<\/b> was observed by naked eye, which could be used as the promising smart materials for the encryption application.","articleNo":"","authorCnList":["张亮"," 李猛"," 高庆宇"," 陈传峰"],"authorEnList":["Zhang Liang"," Li Meng"," Gao Qingyu"," Chen Chuanfeng"],"authorList":["Zhang Liang"," Li Meng"," Gao Qingyu"," Chen Chuanfeng"],"authors":"Zhang Liang, Li Meng, Gao Qingyu, Chen Chuanfeng","authorsCn":"张亮, 李猛, 高庆宇, 陈传峰","authorsEn":"Zhang Liang, Li Meng, Gao Qingyu, Chen Chuanfeng","categoryName":"Note","categoryNameCn":"研究简报","categoryNameEn":"Note","citation":"Zhang Liang, Li Meng, Gao Qingyu, Chen Chuanfeng. Synthesis and Properties of New Organic Luminescent Materials Based on Halogen-Substituted Phthalimides. 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