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Method for the production of losartan

A general formula and compound technology, applied in the field of losartan production, can solve the problems of unreported precursor production, etc.

Inactive Publication Date: 2008-02-27
RATIOPHARM GHBH (DE)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the production of suitable precursors for the synthesis of losartan has not been reported

Method used

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  • Method for the production of losartan
  • Method for the production of losartan
  • Method for the production of losartan

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Experimental program
Comparison scheme
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Embodiment Construction

[0198] Experimental part:

[0199] In the experimental part, the preparation of compounds appearing in Synthetic Schemes A, B or C is further described.

[0200] Experiment description

[0201] Equipment and Reagents

[0202] All dry solvents (CH 2 Cl 2 , THF, Et 2 (O, benzene, toluene, DMF, MeCN) were dried according to standard methods, such as removal of water and oxygen and distillation before use. React under an inert gas atmosphere (N 2 or Ar) and monitored by thin layer chromatography (TLC). Extraction solvents such as diethyl ether, ethyl acetate or chloroform. If not stated otherwise, the extracts were dried eg over anhydrous magnesium sulfate. If necessary, the reaction product is purified, for example, by column chromatography such as petroleum ether (60-90° C.) / ethyl acetate and chloroform / methanol as eluents. If model GF 254 The layer plate is used for thin layer chromatography, and the ethanol solution of iodine or phosphomolybdic acid (phosphormolybdn...

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Abstract

The invention relates to a novel method for the production of losartan, an imidazol derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol and the pharmacologically active salts thereof. The invention also relates to novel intermediate products which are suitable for the production of losartan, and to novel methods for the production of intermediate compounds which are suitable for the production of losartan. One aspect of the invention is a method for the production of a compound of general formula (I), which can arise as an intermediate step in the inventive representation of losartan.

Description

technical field [0001] The present invention relates to a novel process for the production of Losartan, a chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazole- 5-yl) imidazole derivatives of biphenyl-4-]methyl}imidazole, and pharmacologically effective salts thereof. Furthermore, the present invention relates to novel intermediate products suitable for the manufacture of losartan, and novel processes for the preparation of intermediate products suitable for the manufacture of losartan. Background technique [0002] Since losartan has been shown to be an effective agent in the control of hypertension and the resulting disorders in mammals including humans, losartan and its efficient and economical production methods have attracted significant interest. [0003] EP-A-253310 describes losartan and its products for the first time. The synthesis method comprises the necessary step of N-alkylation of imidazole with, for example, a bromomethylbiphenyl derivative ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D233/54C07D403/10C07D257/04C07C251/08
CPCC07D403/10C07C257/14C07D233/64C07D257/04Y02P20/55
Inventor 王亚平李勇刚李玉林郑国军李毅
Owner RATIOPHARM GHBH (DE)
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