Preparation method for clopidogrel intermediate

Abstract

The invention relates to a preparation method for an antiplatelet aggregation medicine clopidogrel optical pure intermediate (S)-2-chlorobenzene glycine or ester. In the method, the (S)-2-chlorobenzene glycine or ester is prepared from the corresponding (S)-phenylglycine or ester through chlorination. By the method, the raw materials and the reagents are low in price and are readily available; the reaction is mild; and the yield is high.

Description

technical field [0001] The invention relates to a preparation method of a compound, in particular to a preparation method of an optically pure intermediate (S)-2-chlorophenylglycine methyl ester or acid of clopidogrel. Background technique [0002] Clopidogrel bisulfate (Clopidogrel Bisulfate), the chemical name is S(+)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothiophene[3,2-c] Pyridine-5) bisulfate of methyl acetate is an anti-platelet aggregation drug. It is a new generation of platelet aggregation inhibitor successfully researched and developed in 1986 by the French Sanofi Sandela Fort Pharmaceutical Company. dimension. The product was first launched in the United States in March 1998, and then entered the markets of Europe, North America, Australia, Singapore and other countries, and was launched in China in August 2001. [0003] There are many domestic and foreign reports about the synthetic route of clopidogrel, but the main synthetic process put into production is to ...

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Problems solved by technology

[0004] As can be seen from the above, the key point of the synthetic route of clopidogrel is the preparation of optically pure (S)-2-chlorophenylglycine methyl ester. Due to the separation, the theoretical maximum yield of the separation is only 50%, which increases the production cost and the three wastes. Although the undesired enantiomer can be recycled by racemization, it is always a challenge to find a more economical method

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