4.6 Article

Synthetic improvements in the preparation of clopidogrel

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ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 11, 期 3, 页码 487-489

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AMER CHEMICAL SOC
DOI: 10.1021/op700025d

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Synthetic improvements in the preparation of clopidogrel are described. The synthesis was accomplished in four steps or one-pot in above 70% overall yield. The process featured PTC catalyzed 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 racemic clopidogrel using L-camphorsulphonic acid in toluene and has been successfully used in a 50-kg pilot test.

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