Synthetic Improvements in the Preparation of Clopidogrel

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• 作者：Lixin Wang ; Jianfen Shen ; Yi Tang ; Yi Chen ; Wen Wang ; Zegui Cai ; and ; Zhenjun Du
• 刊名：Organic Process Research & Development
• 出版年：2007
• 出版时间：May 2007
• 年：2007
• 卷：11
• 期：3
• 页码：487 - 489
• 全文大小：48K
• 年卷期：v.11,no.3(May 2007)
• ISSN：1520-586X

文摘

Synthetic improvements in the preparation of clopidogrel aredescribed. The synthesis was accomplished in four steps or one-pot in above 70% overall yield. The process featured PTCcatalyzed alkaline hydrolysis of the key intermediate 2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)acetonitrile and highly effective kinetic resolution of racemicclopidogrel using L-camphorsulphonic acid in toluene and hasbeen successfully used in a 50-kg pilot test.