Process for synthesizing rebamipide

A synthesis process and technology of rebamipide, applied in the field of synthesis technology of rebamipide, can solve the problems of high impurity content, low product purity, difficulty in obtaining high-purity rebamipide, etc., and achieve the effect of high yield

Inactive Publication Date: 2017-05-10
大桐制药(中国)有限责任公司
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0006] In the product obtained by the above process, the impurity content is high, and the product purity is low, so it is difficult to obtain high-purity rebamipide

Method used

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  • Process for synthesizing rebamipide
  • Process for synthesizing rebamipide
  • Process for synthesizing rebamipide

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Embodiment Construction

[0020] In order to make the purpose, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0021] The synthetic technique of rebamipide, the steps are as follows:

[0022] 1) Add 10g diethyl aminomalonate and 10g triethylamine to 200ml chloroform, stir at room temperature for 30min, then cool to 5°C, add 8.2g 4-chlorobenzoyl chloride dropwise to the reaction solution , after the dropwise addition, react at room temperature for 2 hours, spot the plate to determine the end of the reaction, wash the reaction solution with 200ml of water, 40ml of 5% sodium carbonate sol...

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Abstract

The invention provides a process for synthesizing rebamipide. The process comprises the following steps: taking aminomalonic acid diethyl ester and 4-chlorobenzoyl chloride as raw material substrates so as to prepare an intermediate 4-chlorobenzoyl diethyl aminomalonate; reacting with 4-bromomethylcarbostyril so as to obtain 2-(4-chlorobenzhylamino)-2-ethoxycarbonyl-3-[2(1H)-quinolinone-4-yl] ethyl propionate; and finally, heating and refluxing in a sodium alcoholate solution, concentrating, and re-crystallizing, thereby obtaining the final product. The rebamipide prepared by the process disclosed by the method is high in yield, and the purity can reach 99.2%.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical synthesis, in particular to a synthesis process of rebamipide. Background technique [0002] Rebamipide can improve gastric motility and treat gastric mucosal damage caused by gastric ulcer, acute gastritis, and acute exacerbation of chronic gastritis. Its system name is: 2-(4-chlorobenzamido)-3-[2(1H)-quinolone-4-yl]propionic acid, the CAS registration number is 111911-87-6, and its chemical formula is as follows [0003] [0004] The preparation method of rebamipide has been reported in many patents and literatures, and the common synthesis route disclosed in Japanese patent (JP2008143794A) is as follows: [0005] [0006] In the product obtained by the above process, the impurity content is high, and the product purity is low, so it is difficult to obtain high-purity rebamipide. Contents of the invention [0007] Aiming at the above-mentioned problems, the present invention pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/227
CPCC07D215/227
Inventor 张艳华张媛张荣玉
Owner 大桐制药(中国)有限责任公司
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