Key result
A four-step or one-pot synthesis of clopidogrel achieved an overall yield above 70% and was successfully used in a 50-kg pilot test.
Describes an improved, high-yield synthetic process for the preparation of clopidogrel suitable for large-scale production.
May lower clopidogrel production costs; leaves open effects on access and clinical outcomes.
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(4 H )-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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Wang et al. (2007) studied this question. Synthetic preparation of clopidogrel was evaluated on Overall yield. A four-step or one-pot synthesis of clopidogrel achieved an overall yield above 70% and was successfully used in a 50-kg pilot test.
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