Candesartan Cilexetil and its precursor compound preparation method

Abstract

The invention discloses a ridge-ground shatan ester and making method of prosoma compound, wherein the prosoma compound is 2-ethoxy-1-[[2'-(1-R-tetrazole-5-base) [1, 1'-biphenyl]-4-base] methyl]-1H-benzimidazole-7- carboxyl acid1-(cyclohexaoxy carbonyloxygen) carbethoxy (III), which is reacted by 2-ethoxy-1-(4'-halogenated phenyl) methyl-1H-benzimidazole-7-carboxyl acid1-[[(cyclohexaoxy) carbonyl] oxygen] carbethoxy (I) and 2-(1-R-1H-tetrazoline-5-base) borophenylic acid or 2-(1-R-1H-tetrazoline-5-base) borophenylic acid ester (II) in the organic dielectric and catalyst allowed by Suzuki reaction under soluble alkaline compound condition; hydrolyzing the prosoma compound under acid condition to obtain the medical product.

Description

Technical field

[0001] The present invention relates to the preparation of ester compounds of benzimidazole, in particular to a method for preparing p-candesartan cilexetil and its precursor compounds. Background technique

[0002] Candesartan cilexetil, chemical name: (±)-2-ethoxy-1-[[2′-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]-1H- Benzimidazole-7-carboxylic acid 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester, a benzimidazole compound, is a kind of compound that has been put into use and has ideal antihypertensive and AngII-1 Medicinal drugs with receptor antagonistic activity. Its different preparation routes and methods have been reported in a variety of literature. Among them, in the Chinese patent document with the publication number CN 1207287C, the applicant proposed a method consisting of 2-ethoxy-1-(p-halophenyl)methyl-1H-benzimidazole-7-carboxylic acid The preparation principle and method of 1-[[(cyclohexyloxy)carbonyl]oxy]ethyl ester and protected 5-(2'-halophenyl)-2(1H)te...

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