Z. Xiu-lan
2009
Citations
0
Influential Citations
3
Citations
Journal
Journal of Wuhan Institute of Technology
Abstract
The diethyl-2-(4-chlorobenzoylamino)-2-(1,2-dihydro-2-oxo-4-quinolyl)malonate,an intermediate of ribamipide was synthesized from N-Acetoacetanilide as material.Firstly,4-(bromomethyl)-quinolin-2(1H)-one was obtained by the bromination and cyclization.Then,diethyl-2-(4-chlorobenzamido)malonate was obtained by the acylation of diethyl aminomalonate hydrochloride.Finally,diethyl-2-(4-chlorobenzoylamino)-2-(1,2-dihydro-2-oxo-4-quinolyl)malonate was prepared by alkylation of 4-(bromomethyl)-qui-nolin-2(1H)-one with diethyl-2-(4-chlorobenzamido)malonate,under the conditions which were as follows:the molar ratio of Ⅳ toⅢ to sodium alcoholate was 1∶1∶1.2,the refluxed time was 2 h.The total yield was 63.81%(with N-Acetoacetanilide as the material).