Method for synthesizing diovan

A technology of valsartan and compound is applied in the field of synthesizing valsartan, and achieves the effects of high yield, low price, and avoiding excessive heavy metal tin.

Active Publication Date: 2008-09-24
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The technical problem to be solved by the present invention is to overcome the shortcoming of the above-mentioned valsartan synthesis step, cancel the use of halogenated alkyl tin compounds to pa

Method used

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  • Method for synthesizing diovan
  • Method for synthesizing diovan

Examples

Experimental program
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example 1

[0015] Add 50L of drinking water, then add 25kg of potassium carbonate and stir until it is dissolved, then add 20kg of condensate hydrochloride and 150L of toluene, and stir until it is dissolved. Control the temperature at 20-30°C and start adding dropwise the mixture of 9kg valeryl chloride and 25L toluene, the dropwise addition is completed in about 2 hours, then keep the temperature at 20-30°C and stir the reaction for 1 hour, let stand to separate and separate the lower water layer, The organic layer was washed with saturated brine. The saline layer was separated, and the organic layer (pentanoylate solution) was set aside. Use the pentanoyl compound solution prepared in the previous step, add 7.3Kg of sodium azide and 17.8kg of triethylamine hydrochloride, stir evenly, heat to reflux, react for 20 hours, cool to 30°C after reflux, and then add saturated saline 50L, let it stand for stratification. The brine layer was removed, and the organic layer was washed with an a...

example 2

[0017] Except replacing the salt of wormwood in the example 1 with sodium carbonate, all the other are the same as the example 1, and the yield is 75%.

example 3

[0019] Except replacing the potassium carbonate in example 1 with sodium bicarbonate, all the other are with example 1.

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Abstract

The present invention provides an improved method used for synthesizing valsartan. No tin compounds are required in the reaction. In the method, the condensate of N-[(2'-cyano-1, 1'- biphenyl-4-group)-alkyl]-L-valine ester is used as raw material. And the method comprises valerylation and synthesis of the valsartan. The method has the advantages of easily available raw materials, simple operation, no environmental pollution, high yield, low cost, and suitability for large-scale industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicines. Specifically relates to an improved method for synthesizing valsartan without tin compounds participating in the reaction. Background technique: [0002] Valsartan is an effective chemical synthetic drug for the treatment of hypertension, its chemical name: (S).N-(1-oxopentyl)-N-[4-[2-(1H-tetrazolium- 5-yl)phenyl]benzyl]-L-valine, English name (S)-N-pentanoyl-N-[[2′-(1H-tetrazole-5-yl)[1,1′-biphenyl ]-4-yl]methyl]-L-valine (valsartan), its synthesis method is mainly divided into condensation products (N-[(2'-cyano-1,1'-biphenyl-4-yl) alkyl] The synthesis of -L-valine ester) (hydrochloride) (containing ester protection), the synthesis of valsartan (containing valerylation) two parts; Cyano-4'-bromomethylbiphenyl as raw material, obtained by condensation with carboxyl-protected L-valine, and the second is 2-cyano-4'-formylbiphenyl as raw material and carboxyl-protected It is obtained by conde...

Claims

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Application Information

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IPC IPC(8): C07D257/04
Inventor 王礼权陈伟刘大鹏
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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