Clopidogrel is a new generation of platelet aggregation inhibitors, mainly used to treat thrombotic complications. CPG105, chemical name: methyl (S)-2-(2-(thiophene-2-) ethylamino)-2-(2-chlorophenyl)-acetate is a key intermediate of clopidogrel. After long-term research, this project has developed a CPG105 green production process that is technologically advanced, low-cost and suitable for industrialization. It has the advantages of stable process, high yield and environmentally friendly. It has applied for 5 China patent protection.  

 In this project, o-chlorophenylglycine (1) was used as the starting material to synthesize o-chlorophenylglycine methyl ester (2) through esterification, and then subjected to dynamic kinetic resolution of tartaric acid to prepare (S)-(+) o-chlorophenylglycine methyl ester-L-tartrate salt (3), which was directly condensed with thiophene-2-ethyl p-toluenesulfonate compound without separation to obtain CPG105 with high optical purity.

 The production process of this project is leading in China, with mature technical conditions and can be industrially produced. The product quality is stable and the optical purity is above 99.5%, which meets the requirements of high-quality customers. Clopidogrel produced from this intermediate meets USP34 and other quality standards.

This process patent CN200810033932 has been authorized.