Method for preparing sartan drug main ring 5-(4'-formyl biphenyl-2-group)-1H-tetrazole treating hypertension

Abstract

The invention belongs to drug synthesis, particularly relates to the main ring of Sartan drug for the treatment of the hypertension i.e. 5-(4'-formyl biphenyl-2-base)-1H-tetrazole. The preparation method comprises the following procedures, bromination, esterification, cyclization, hydrolysis and oxidation. Utilizing the triethylamine hydrochloride to serve as the catalyst, the method of the invention inhibits the side reaction, promotes the purity and the yield of the product, avoids the residue of the poisonous matter in the drug intermediate, reduces the waste discharge, realizes the clean production and protects the environment.

Description

technical field

[0001] The invention relates to a preparation method of 5-(4'-formylbiphenyl-2-yl)-1H-tetrazolium, which is the main ring of sartan drugs for treating hypertension, and belongs to the field of chemical pharmacy. Background technique

[0002] The main ring used in the synthesis of sartan antihypertensive drugs is mainly N-triphenylmethyl-5-(4'-bromomethylbiphenyl-2-yl)-1H-tetrazolium (I). Due to the difficulty in preparation and purification of this intermediate, its price has remained high. In order to further reduce the cost of drug production and improve the quality of drugs, the new intermediate 5-(4'-formylbiphenyl-2-yl )-1H-tetrazolium (II) was successfully developed.

[0003]

[0004] 5-(4'-Formylbiphenyl-2-yl)-1H-tetrazolium (II) is a new type of pharmaceutical intermediate, which can be used to produce multiple sartan antihypertensive drugs, such as valsartan , losartan, irbesartan, olmesartan, and candesartan. Compared with the traditional sart...

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