Synthetic process for candesartan cilexetil

A technology for the synthesis of candesartan cilexetil, which is applied in the field of medicine, can solve problems such as difficult implementation of the process, low production efficiency, and complicated production process, so as to improve the single-pass conversion rate and product yield, and improve work efficiency , to overcome the effect of more processes

Inactive Publication Date: 2016-06-08
QINGDAO SHOUTAI AGRI SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the current synthesis process of candesartan cilexetil, the technical process is not easy to implement, the generated candesartan cilexetil has low purity, the single-pass conversion rate of reactants is low, the production process is complicated and pollutes the environment relatively, the production efficiency is low and the cost is low. high cost

Method used

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Experimental program
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Effect test

Embodiment

[0011] The synthetic technique of the candesartan cilexetil of the present embodiment comprises the following steps:

[0012] (1) With ethyl 1-[(2'-cyano-1,1'-biphenyl-4-yl)methyl]-2-ethoxy-7-benzimidazolecarboxylate and azide Sodium chloride is used as a raw material, N,N-dimethylformamide is used as a solvent, MCl is used as a catalyst, and the reaction is carried out at 150° C. for 30 hours;

[0013] (2) Cool and depressurize to remove N,N-dimethylformamide, wash with toluene or xylene, and adjust the pH to 6 with 1N-HCl-;

[0014] (3) Solids are precipitated, filtered, and recrystallized from methanol to obtain candesartan cilexetil, wherein M is a metal or ammonium cation.

[0015] The synthesis process of candesartan cilexetil does not require further processing, the process is simple, the data is accurate and easy to measure, and the process flow is easy to implement.

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PUM

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Abstract

The invention discloses a synthetic process for candesartan cilexetil. The synthetic process synthesizes candesartan cilexetil under a temperature of 150 to 170 DEG C with 1-[(2'-cyano-1,1'-biphenyl-4-yl)methyl]-2-ethoxyl-7-benzimidazole carboxylic acid ethyl ester and sodium azide as raw materials, N,N-dimethyl formamide as a solvent and MCl as a catalyst, wherein M is an alkali metal or an ammonium cation. The synthetic process provided by the invention has the following advantages: the used catalyst is cheap and non-toxic or low-toxicity, so production cost and environmental treatment cost are reduced; meanwhile, reaction after-treatment is simple, and yield is high, so the process is favorable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a synthesis process of candesartan cilexetil. Background technique [0002] Candesartan cilexetil is indicated for essential hypertension. Candesartan cilexetil is rapidly hydrolyzed into the active metabolite candesartan in the body. Candesartan is a selective angiotensin II receptor (AT1) antagonist that antagonizes vascular tension by binding to vascular smooth muscle AT1 receptors. The vasoconstriction effect of factor II reduces the peripheral vascular resistance. In the current synthesis process of candesartan cilexetil, the technical process is not easy to implement, the generated candesartan cilexetil has low purity, the single-pass conversion rate of reactants is low, the production process is complicated and pollutes the environment relatively, the production efficiency is low and the cost is low. The cost is high. Contents of the invention [0003...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/10
Inventor 张晶
Owner QINGDAO SHOUTAI AGRI SCI & TECH CO LTD
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