Practical Synthesis of TJAB1099: An Effective Anti EV71 Inhibitor

被引：1
作者：
He, Wanli [1 ,3 ]
Zhao, Yangyang [1 ,3 ]
Mao, Yonghong [1 ]
Zhao, Peipei [1 ]
Wang, Ying [1 ,3 ]
Cai, Yan [1 ,2 ]
机构：
[1] Tianjin Int Joint Acad Biomed, Tianjin 300457, Peoples R China
[2] Nankai Univ, State Key Lab Med Chem Biol, Tianjin 300071, Peoples R China
[3] Nankai Univ, Coll Pharm, Tianjin 300071, Peoples R China
来源：
CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2017年 / 37卷 / 09期
关键词：
enterovirus; 71; inhibitor; synthetic method; HUMAN ENTEROVIRUS; CAPSID-BINDING; FOOT; HAND;
D O I：
10.6023/cjoc201704002
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
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.
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收藏
页码：2361 / 2368
页数：8
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