op700025d_si_002.pdf (457.96 kB)
Synthetic Improvements in the Preparation of Clopidogrel
journal contribution
posted on 2007-05-18, 00:00 authored by Lixin Wang, Jianfen Shen, Yi Tang, Yi Chen, Wen Wang, Zegui Cai, Zhenjun DuSynthetic 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.