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Improved preparation method of rebamipide intermediate

A technology of intermediates and reaction time, applied in the direction of organic chemistry, etc., can solve the problems of low reaction yield, low product purity, and increased cost, and achieve the effects of high product purity, improved product yield, and easy operation.

Inactive Publication Date: 2010-10-27
SHAANXI DASHENG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

Such disadvantages are that raw materials and solvents must be strictly anhydrous, and the reaction process must be strictly forbidden to bring in water; due to the use of metallic sodium, it is very dangerous; and the reaction time is 6-18 hours, and the reaction yield is 30-45%. The product has low purity and needs to be refined again
In this way, the cost is correspondingly increased a lot

Method used

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  • Improved preparation method of rebamipide intermediate
  • Improved preparation method of rebamipide intermediate
  • Improved preparation method of rebamipide intermediate

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Abstract

The invention provides an improved preparation method of a rebamipide intermediate. An intermediate (4) is obtained by condensation reaction of an intermediate (2) and an intermediate (3) in DMF (Dimethyl Formamide) / NaOH, wherein the reaction time is 5-7h, the yield is 85-92 percent, and the product purity is above 98.5 percent. The method has mild reaction condition as well as simple and convenient operation, can remarkably improve the operability on the product yield and industry and is beneficial to industrial production.

Description

technical field The invention provides a method for preparing an intermediate of rebamipide, a medicine for treating gastric ulcer. Background technique The gastric mucosal protective agent rebamipide (1) was developed by Otsuka Pharmaceutical, and its chemical name is: 2-(4-chlorobenzamido)-3-[2(1H)-quinolone-4-yl]propane Acid, listed in Japan in 1990, is now widely used in Europe, America and other countries. The anti-ulcer mechanism of this drug is different from that of H2 receptor antagonists and proton pump inhibitors. It mainly promotes the healing of peptic ulcer by increasing gastric mucosal blood flow, prostaglandin E2 synthesis, gastric mucus secretion, and scavenging oxygen free radicals. Improve inflammation, reduce ulcer recurrence, and improve the eradication rate of Helicobacter pylori. In the production of rebamipide (1), intermediate (4) is an essential key step. US6680386, US2007249835, JP-A-60-19767, etc. all use intermediate (2) and intermediate (3...

Claims

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Application Information

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IPC IPC(8): C07D215/227
Inventor 白振奎杨刚利
Owner SHAANXI DASHENG PHARMA TECH
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