钙拮抗剂拉西地平的合成新工艺  

New synthetic route for lacidipine

作　　者：黄河清[1] 李树春[1] 王安邦[1] 蔡孟深[1] 李中军[1] 

机构地区：[1]北京大学药学院化学生物学系,北京100083

出　　处：《中国药物化学杂志》2004年第6期365-367,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的完成钙拮抗剂拉西地平合成的新工艺。方法以邻苯二甲醛、β 氨基巴豆酸乙酯、三苯基亚膦基乙酸叔丁酯为原料 ,采用常规的化学合成法合成。结果采用先形成二氢吡啶环 ,再通过Wittig反应制备烯烃双键的顺序 ,拓展了拉西地平合成的新工艺。 结论新工艺与专利文献相比 ,具有收率高、操作简便的特点 ,更适于工业化生产。Aim To establish a new method for the synthesis of lacidipine.Method To form the 1,4 dihydropyridine ring at first and to construct the double bond of the acrylic ester side chain,exploiting phthalaldehyde,ethyl 3 aminocrotonate and diethyl t butoxycarbonylmethyl phosphonate as the starting materials.Lacidipine was prepared through the new strategy.Results and conclusion Lacidipine was synthesized in a good yield through a 2 step procedure.It is different from the patent synthetic procedure for lacidipine and it is a new synthetic procedure with better yield and would be suitable for industrial manufacture.

关 键 词：药物化学 工艺改进 化学合成 钙拮抗剂 拉西地平 

分 类 号：TQ463[化学工程—制药化工]