阿折地平的合成工艺改进  

Improved synthesis of azelnidipine

作　　者：刘剑峰[1] 韩建奎[1] 侯桂华[2] 黄亚丽[1] 徐文方[3] 

机构地区：[1]山东大学齐鲁医院,山东济南250012 [2]山东大学医学院,山东济南250012 [3]山东大学药学院,山东济南250012

出　　处：《中国药物化学杂志》2010年第3期192-194,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进抗高血压药物阿折地平的合成工艺。方法以二苯甲胺和环氧氯丙烷为起始原料,经取代、酯化、酸化、缩合等反应制得抗高血压药物阿折地平。结果与结论目标化合物的结构经1H-NMR谱和质谱确证。总收率为30.88%,比文献收率提高了10.62%。改进后的方法操作简便,有利于工业化生产。Aim To improve the synthetic procedure of azelnidipine.Methods Azelnidipine was synthesized from aminodiphenylmethane and epichlorohydrin via substitution,esterification,acidification,condensation,etc.Results and conclusion The structure of target compound was confirmed by ^1H-NMR,MS.The overall yield of the process is 30.88%.Compared with the reported method,the overall yield is 10.62% higher.This synthetic process is suitable for industrial preparation by its convenient operation.

关 键 词：二苯甲胺 环氧氯丙烷 阿折地平 抗高血压药 

分 类 号：TQ463.53[化学工程—制药化工]