Preparation method of rebamipide intermediate

A technology of volume ratio and structural formula, which is applied in the field of preparation of the key intermediate of rebamipide, 2-amino-3-[2(1hydrogen)-quinolon-4-yl]propionate, can solve the problem of low yield , incomplete reaction, easy flushing and other problems
CN102153512BActive Publication Date: 2013-03-27JIANGXI SYNERGY PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGXI SYNERGY PHARMA
Publication Date
2013-03-27

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Abstract

The invention discloses a preparation method of a compound disclosed as a structural formula 1. The compound is a key intermediate for synthesizing rebamipide. The method comprises the following steps: I. in the presence of alkali, reacting a compound disclosed as a structural formula 2 with a compound disclosed as a structural formula 3 in C1-C4 fatty alcohol; after the reaction finishes, regulating the pH value to higher than or equal to 8 with acid, adding water, and filtering to obtain a compound disclosed as a structural formula 4; and II. in an organic solvent, reacting the compound disclosed as the structural formula 4 in step I with acid at 30-130 DEG C, after the reaction finishes, cooling to crystallize, and filtering to obtain the compound disclosed as the structural formula 1, wherein the acid is composed of organic acid and inorganic acid in any ratio, the organic acid is one or more of formic acid, acetic acid, propanoic acid and oxalic acid, and the inorganic acid is one or more of hydrochloric acid, sulfuric acid, phosphoric acid and hydrobromic acid. The invention solves the problems of high material wash-away tendency and low yield in the prior art.
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Description

technical field

[0001] The invention belongs to the field of organic chemistry, and in particular relates to a preparation method of 2-amino-3-[2(1hydrogen)-quinolone-4-yl]propionate, a key intermediate 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 systematic name is: 2-(4-chlorobenzamido)-3-[2(1hydrogen)-quinolone-4-yl]propionic acid, and its CAS registration number is 111911-87-6. The key intermediate in the synthesis of rebamipide is 2-amino-3-[2(1hydrogen)-quinolone-4-yl] propionate hydrochloride, except for hydrochloride, the 2-amino-3-[2 (1H)-quinolone-4-yl] propionic acid sulfate, phosphate, hydrobromide, etc., can also be used as intermediates of rebamipide, and the general structural formula of the above-mentioned various salts is shown in 1 .

[0003]

[0004] For the preparation method of 2-amino-3...

Claims

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