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%.
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Paragraph 0025; 0026; 0027
(2017/08/28)
Process for preparing 2-(4-chlorobenzolamino)-3[ (1h)-quinolinon-4-yl] propionic acid
The invention relates to a novel method for preparing 2-(4-chlorobenzoylamino)-3-[2(1H)-quinolinon-4-yl]propionic acid, also known as Rebamipide represented by the formula I and useful for treatment of peptic ulcer from alkyl 2-(4-chlorobenzoylamino)-2-alkoxycarbonyl-3-[2(1H)-quinolinon-4-yl]propionate represented by the formula II in the presence of a base solution for hydrolysis and decarboxylation to remove a carboxyl group.
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(2008/06/13)
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