Preparation method of gefarnate

A technology of Gefarin and triethyl orthoacetate, applied in the field of medicine, can solve the problems of high pollution degree of Gefaryl, difficult to remove toxicity, easy volatilization, etc., to reduce the generation of toxic by-products and improve the utilization rate of raw materials , the effect of low solvent toxicity

Active Publication Date: 2010-08-18
海南新世通制药有限公司
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Problems solved by technology

Chinese patent CN101475476A discloses a method for synthesizing gefar esters. The by-products of the first step reaction and the second step reaction of this method all contain methanol. Methanol is highly toxic and volatile, and the human body will inhale methanol vapor. Causes damage to the respiratory mucosa and affects vision. At the same time, the solvent N, N dimethylformamide (DMF) used in the second step reaction is also highly toxic and difficult to remove.
Therefore, adopting said method to prepare gefar esters has a high degree of pollution to the environment

Method used

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  • Preparation method of gefarnate
  • Preparation method of gefarnate
  • Preparation method of gefarnate

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Abstract

The invention provides a preparation method of gefarnate, comprising the following steps: nerolidol, triethyl orthoacetate and acid catalyst are mixed and heated, thus obtaining a first intermediate product; the first intermediate product is added to ethanol solution of alkali and heated, thus obtaining a second intermediate product; the second intermediate product is dissolved by water, and then the PH value of the solution is regulated to 1-4, thus obtaining a third intermediate product; and geraniol is added after the third intermediate product is dissolved by organic solvent and heated, thus obtaining the gefarnate. By adopting the method in the invention to prepare the gefarnate, the solvent used in the production process and the produced by-products have low toxicity, and the ethanol which is produced in the reaction can be reused, thus reducing the pollution to the environment and enhancing the utilization ratio of raw materials.

Description

A kind of preparation method of gefar ester technical field The invention relates to the field of medicine, in particular to a preparation method of gefarate. Background technique The chemical name of Gefarnate is (4E, 8E)-5,9,13-trimethyl-4,8,12-tetratrienoic acid-(2E)-3,7-dimethyl-2 , 6-octadienyl ester, its chemical structural formula is shown in formula VII. Gefate is a compound with an isoprene structure and is a fat-soluble oily substance. Gefate can adjust gastrointestinal function, enhance the protective effect of gastric mucosa, and can control gastric acid, gas, bloating and pain, so it is widely used in the treatment of flatulence, gastric ulcer and duodenal ulcer, etc. Gastrointestinal disease. Chinese patent CN101475476A discloses a method for synthesizing gefar esters. The by-products of the first step reaction and the second step reaction of this method all contain methanol. Methanol is highly toxic and volatile, and the human body will inhale methan...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/587C07C67/08
Inventor 陈精慧蔡郴花李仁祥张燕冯新侠黄国雁
Owner 海南新世通制药有限公司
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