抗溃疡药马来酸伊索拉定的合成新方法

New synthetic method of the antiulcer drug irsogladine maleate

采用新的合成路线制备新型抗溃疡药马来酸伊索拉定 (irsogladinemaleate) ,以对二氯苯为起始原料 ,经乙酰化、溴仿反应、氰化、环合、成盐五步反应制得目标化合物 ,其结构经谱图确证。该法原料价廉易得 ,三废污染少 ,总收率为 31 2 % 。

Irsogladine maleate as an antiulcer drug was synthesized according to a new route. p Dichlorobenzene which is more inexpensive and more easily available was used as the starting material through acetylation,bromoformation,cyanidation,cyclization and saltation steps to gain the target compound.The structure of the final compound was confirmed by IR, 1H NMR,MS and elemental analysis.The overall yield was 31 2% and it was similar to that in the former report.