| 摘要 |
PURPOSE: A process for preparing carbostyrile derivative having therapeutic effect on ulcer is provided, thereby the carbostyrile derivative can be cheaply prepared in higher yield without by-products. CONSTITUTION: The process for preparing carbostyrile derivative comprises the steps of: reacting aminomalonate of dialkyl phenyl derivative represented by formula(2) with 4-halomethyl-1H-quinoline-2-one of formula(3) to prepare 2-(benzoylamino)- 2-(2-oxo-1,2-dihydroquinoline-4-ylmethyl) malonic acid ester of formula(4); and selectively decarbonating the compound of formula(4) to prepare 2-(benzoylamino)- 3-(2-oxo-1,2-dihydroquinoline-4-yl) propionic acid derivative, in which R is phenyl, 4-chlorophenyl, 4-methoxyphenyl; R1 and R2 are methyl or ethyl; and X is chlorine or bromide.
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