引用本文:
周懿波, 刘天麟. 有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成[J]. 应用化学,
2001, 18(2): 92-95.
Citation: ZHOU Yi-Bo, LIU Tian-Lin. Synthesis of Bioactive Pyridazinone-Carbamate Derivatives[J]. Chinese Journal of Applied Chemistry, 2001, 18(2): 92-95.
Citation: ZHOU Yi-Bo, LIU Tian-Lin. Synthesis of Bioactive Pyridazinone-Carbamate Derivatives[J]. Chinese Journal of Applied Chemistry, 2001, 18(2): 92-95.
有生物活性的哒嗪酮-氨基甲酸酯类衍生物的合成
摘要:
从2-取代-4,5-二氯哒嗪酮(1)出发,使2-取代-4-氯-5-羟基哒嗪酮(2)与溴乙基氨基甲酸酯反应合成含哒嗪酮的氨基甲酸酯类化合物(5a,5b).将化合物1与乙醇胺反应制得2-取代-4-氯-5-(2-氨基乙氧)哒嗪酮(3),化合物3与氯甲酸酯反应得到5a~5l.化合物3催化加氢生成2-取代-5-(2-氨基乙氧)哒嗪酮(4).化合物4与氯甲酸酯在-10~-5℃反应得到化合物(6a~6d),在0~15℃反应得到相应N,N-二甲酸酯化合物(7a,7b).探讨了中间体3与4的反应活性.生物活性测试结果表明其中一些化合物具有较好的杀菌活性.
English
Synthesis of Bioactive Pyridazinone-Carbamate Derivatives
Abstract:
Pyridazinone-carbamate derivatives 5a~5l were synthesized starting from 2-substituted-4,5-dichloro pyridazinones 1 via two routes. One is that 2-substituted-4-chloro-5-hydroxyl pyrida-zinones 2 reacted with U-bromoethyl carbamates to afford compounds 5a and 5b. The other is that 2-substituted-4-chloro-5-(2-amino ethyloxyl)pyridazinones 3 obtained from the reaction of 1 with amino ethanol, reacted with chloroformate to give 5a~5l. Furthermore, the catalytic hydrogenation of 3 gave 2-substituted-5-(2-amino ethyloxyl)pyridazinones 4, which reacted with chloromates to produce compounds 6a~6d at temperatures between -10~-5℃, and to N,N-dicarbamates 7a and 7b at 0~15℃. The reactivity of intermidiates 3 and 4 was also discussed. The preliminary bioassay indicated that almost all of the compounds showed fungicidal activities.
-
Key words:
- pyridazinone
- / carbamate
- / derivative
- / synthesis
-
-
扫一扫看文章
计量
- PDF下载量: 1
- 文章访问数: 321
- HTML全文浏览量: 63
下载:
