Hu Jia-peng
2012
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Zhejiang Chemical Industry
Abstract
(S)-methyl 2-amino-2-(2-chlorophenyl)acetate is obtained from racemic 2-amino-2-(2-chlorophenyl) acetic acid through esterification and optical resolution,which was subjected to condensation reaction with 2-(thiophen-2-yl)ethyl 4-methyl benzene sulfonate to afford the critical intermediate(S)-methyl 2-(2-chlorophenyl)-2-(2-(thiophen-2-yl)ethylamino) acetate.The cyclization of(S)-methyl 2-(2-chlorophenyl)-2-(2-(thiophen-2-yl)ethylamino) acetate with paraformaldehyde in the presence of anhydrous formic acid provided the Clopidogrel bisulfate.For this synthesis pathway,there are some advantages such as readily available starting material,moderate condition,high yield and good quality.This process is suitable for industrialization.