Improved method for synthesizing valsartan

A compound, the technology of valine alkyl ester, applied in the direction of organic chemistry, can solve the problems of low yield, difficult to reduce the content of optical isomers, difficult to control, etc.
CN101817795AActive Publication Date: 2010-09-01ZHEJIANG MENOVO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG MENOVO PHARMA
Publication Date
2010-09-01

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Abstract

The invention provides an improved method for synthesizing valsartan. The valsartan synthesized by the method can be further purified to give high-purity valsartan. In the method, tin compounds are not used, N-[(2'-cyano-1,1'-biphenyl-4-yl)alkyl]-ester L-valine monohydrochloride is used as a raw material, pentaacylation, diazotization and saponification are performed to obtain the valsartan, a crystallization process is controlled and thus the high-purity valsartan is obtained. The method has the advantages that: the operation is simple; the yield is high; the product purity is high; and the industrial production is easy.
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Description

(1) Technical field

[0001] The invention relates to an improved method for synthesizing valsartan, belonging to the fields of chemical industry and chemical medicine. (2) Background technology

[0002] Valsartan (Valsartan), Chinese name (S)-N-(1-pentanoyl)N-[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-L-valerian Amino acid, a non-peptide angiotensin II receptor antagonist (ARB), was first launched in Germany after being successfully developed by Swiss Novartis. It was approved by the US FDA in December 1996 and launched in the US in 1997 under the product name Diovan. In 1998, Novartis’ valsartan was registered in China under the product name Diovan. Valsartan's US patent will expire on March 12, 2012.

[0003] The preparation method mentioned in U.S. Patent US5399578A is: compound 4 (N-[(2'-cyano-1,1'-biphenyl-4-yl) alkyl]-L-valine methyl ester hydrochloride) Mixed with dichloromethane and triethylamine, and then reacted with valeryl chloride to obtain compound 5 (N-(1-pentan...

Claims

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