氨氯地平苯磺酸盐的合成

Synthesis of AmLodipine Besylate

以乙醇胺和三苯基氯甲烷为起始原料,经氨基保护、取代、缩合、加成、水解和成盐反应,以43%的总收率制得氨氯地平苯磺酸盐;其中部分中间体和目标化合物的结构经1HNMR和MS等进行了表征。该合成路线的总收率与Pfizer公司2003年报道的第二代合成工艺的总收率持平,且具有原料易得、操作简便等特点。

The synthetic method of a calcium-channel antagonist amLodipine besylate was introduced in this paper.AmLodipine besylate was synthesized via protection,replacement,condensation,addition,hydrolysis and saltification from triphenyl chloride methane and monoethanol amine.The yield of all synthetic steps is 43%.The partly intermediate product and the target product were identified by 1HNMR and MS.The yield of this synthetic process,featured with cheap reagents and simple operations,is not less than the second synthetic routes reported by the Pfizer Company in 2003.