Citation: He Wanli, Zhao Yangyang, Mao Yonghong, Zhao Peipei, Wang Ying, Cai Yan. Practical Synthesis of TJAB1099:An Effective Anti EV71 Inhibitor[J]. Chinese Journal of Organic Chemistry, ;2017, 37(9): 2361-2368. doi: 10.6023/cjoc201704002 shu

Practical Synthesis of TJAB1099:An Effective Anti EV71 Inhibitor

He Wanli ^a,c ,
Zhao Yangyang ^a,c ,
Mao Yonghong ^a ,
Zhao Peipei ^a,, ,
Wang Ying ^a,c,, ,
Cai Yan ^a,b,,

a.
Tianjin International Joint Academy of Biomedicine, Tianjin 300457
b.
State Key Laboratory of Medicinal Chemical Biology, Nankai University, Tianjin 300071
c.
College of Pharmacy, Nankai University, Tianjin 300071

Corresponding author: Zhao Peipei, apple.12.26@163.com Wang Ying, wangying1412@163.com Cai Yan, caiyan_86@163.com
Received Date: 1 April 2017
Revised Date: 26 April 2017
Available Online: 10 September 2017
Fund Project: the Science and Technology Planning Project of Tianjin City 13ZCZDSY04200the Science and Technology Planning Project of Tianjin City 14ZCZDSY00039Project supported by the State Key Laboratory of Medicinal Chemical Biology Open Fund (Nankai University) (No. 201602003), and the Science and Technology Planning Project of Tianjin City (Nos. 13ZCZDSY04200, 14ZCZDSY00039)the State Key Laboratory of Medicinal Chemical Biology Open Fund (Nankai University) 201602003

Figures(5)

Enterovirus 71 (EV71) is the main pathogen caused Human Hand, Foot and Mouth Disease (HFMD) in China. It not only caused mild case, but also serious case. However, no effective commercialize drugs for the treatment of HFMD were available nowadays. TJAB1099 is an effective EV71 inhibitor which was designed based on the capsid protein VP1 of EV71. The preclinical study has revealed that it owns excellent druggability. Here an practical synthesis of TJAB1099, initiated with 2-amino-4-bromide pyridine is reported. The total synthetic steps are six and its total yield is 12%. The purity of TJAB1099 is more than 99%, and silic gel chromatography is not required in the whole process. This synthetic method has been examined by hectogram level starting feeding for several times, and the total yield and the content of impurities are stable. This method could meet the need of the inhibitor amount for the preclinical study, and it could lay the foundation of further large scale synthesis.
- enterovirus 71,
- inhibitor,
- synthetic method
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