Method for purifying rebamipide crude product

A technology of rebamipide and purification method, which is applied in the field of synthesis and separation of organic compounds, and can solve the problems that restrict the preparation and use of rebamipide gastric mucosal protective agent, and the purity is difficult to exceed 99.5%.

Inactive Publication Date: 2009-06-24
苏州天马医药集团天吉生物制药有限公司
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  • Abstract
  • Description
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Problems solved by technology

In the prior art, the crude product of rebamipide is usually purified by the method of decolorization and refining, but the purity of the purified rebamipide is difficult to exceed 99.5%. preparation and use

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  • Method for purifying rebamipide crude product
  • Method for purifying rebamipide crude product
  • Method for purifying rebamipide crude product

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Embodiment Construction

[0019] The purpose of the present invention is to purify the crude rebamipide, and through analyzing the structure and cause of the stubborn impurity, the solution is pointedly proposed, and a better purification effect is achieved.

[0020] As mentioned in the background art, the inventors of the present application prepared crude rebamipide through various methods, and when it was decolorized and refined, the purity was difficult to exceed 99.5%. Through RP-HPLC impurity separation, and mass spectrometry, infrared spectrum and proton spectrum comprehensive analysis research, find that two kinds of impurities that are difficult to remove are two kinds of substances shown in formula (a) and (b); And, these two kinds of substances are very To a large extent, it comes from the decolorization and refining process. That is: during the refining process, on the one hand, purified rebamipide (vi) is obtained, and on the other hand, impurities (a) and (b) that are difficult to remove ...

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Abstract

The invention relates to a purifying method for a Rebamipide crude product. Alkaline is added in alcohol-water mixed solvent to dissolve the Rebamipide crude product. Then, activated carbon is added for decolorizing. Concentrated hydrochloric acid is added dropwise, pH is regulated to 2-3, solids are precipitated, and purified Rebamipide is obtained after filtering and drying. During the process, the mol ratio of the added amount of alkaline to the Rebamipide is controlled to be less than 3 to 1. And the operational temperature during the alkaline adding for dissolution and the acid adding for crystallization is controlled at 150 DEG C; therefore; the ring cleavage reaction of quinolone is inhabited and the generation of two impurities which are similar in structure with Rebamipide is reduced. Rebamipide with the purity of higher than 99.5 percent is obtained. Conditions are provided for improving the application degree of Rebamipide in pharmaceutical aspects of gastric mucosal protective drugs, etc.

Description

[0001] Involved areas [0002] The invention relates to the production of rebamipide, in particular to the purification of crude rebamipide, and belongs to the technical field of synthesis and separation of organic compounds. Background technique [0003] Rebamipide is a quinolone compound, its chemical name is: 2-(4-chlorobenzamido)-3-(1,2-dihydro-2-oxo-4-quinolyl)propionic acid , can be used to prepare gastric mucosal protective agent, has the effect of preventing ulcer and promoting ulcer healing, can increase gastric mucosal blood flow, synthesis of prostaglandin E2 and gastric mucus secretion, remove oxygen free radicals, promote healing of peptic ulcer and inflammation improve. [0004] [0005] Formula (vi) is the structural formula of rebamipide, and its crude product (vi') is usually synthesized by the following three methods, and the obtained crude product of rebamipide is further purified, and then used to prepare gastric mucosal protective agents and the like....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/227A61P1/04
Inventor 徐仁华岳年春徐斌
Owner 苏州天马医药集团天吉生物制药有限公司
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