Method for refining Valsartan containing more than 10% of isomer

Abstract

The invention discloses a method for refining Valsartan containing higher isomer impurity, namely Valsartan containing more than 10% (HPLC detection peak area method) of N isomer is refined by adopting butanone or the mixture solvent of butanone and esters and ethers, the N isomer can be remarkably reduced to about 1.0%, and the yield can be as high as more than 50%.

Description

technical field

[0001] The invention relates to a method for refining valsartan containing higher isomers (more than 10%), and belongs to the field of medicine and chemical industry. Background technique

[0002] Valsartan (valsartan), chemical name N-(1-oxopentyl) N-[4-[2-(1H-tetrazol-5 base) phenyl] benzyl]-L-valine, is the following Another new type of antihypertensive drug after calcium ion channel blockers and angiotensin converting enzyme inhibitors (ACEI), it is an angiotensin II (angiotensin II) AT receptor antagonist, avoiding calcium antagonists and ACEI It has the advantages of significant curative effect and good tolerance.

[0003] During the synthesis of valsartan, due to the influence of reaction conditions, some products will racemize, thereby converting from L-form to D-form isomer. If the D-type isomer is higher than 10% (HPLC detection peak area method), it needs to be refined repeatedly with ethyl acetate, which will inevitably cause cost increase, and ...

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