钙拮抗剂拉西地平的合成新工艺

New synthetic route for lacidipine

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.