新一代心血管药物氨氯地平的合成.pdf

2006 1 2 1 Jan. 2006 CHEMICAL INDUSTRY AND ENGINEERING Vol. 2 No. 1 : 1004- 95 ( 2006) 01- 0088- 05 刘鹤超, 冯亚青 ( , 00072) : 介绍了新 一代高效心血管药物氨氯地平的合成方法, 以及国内外的生产现状 点介绍了 氨氯地平合成过程中的关键步骤: 二氢吡啶环的两类成环反应, 即Hantzsch 反应和Michael 加成成 环反应并通过具体实例比较了不同氨基保护的Hantzsch 反应合成路线和Michael 加成成环反应 合成路线的优劣势及工业应用前景 : 氨氯地平; 合成; 1, 4-二氢吡啶 : R972 : A Synthesis of New Ant-i Hypertensive Drug of Amlodipine LIU He-chao, FENG Ya-qing (School of Chemical Engineering and Technology, Tianjin University, Tianjin 00072, China) Abstract: In this paper, various synthesizing method, medical mechanism, productive situation at home and abroad of amlodipine are reviewed. The key step in the synthesis of amlodipine, cyclization of the 1, 4- dihydropyridine by Michael addition reaction and Hantzsch reaction in which different amine protective groups were used, are illustrated in details. By comparing the advantages and disadvantages of the two different processes, the feasibilities of industrial application is discussed. Key words: amlodipine; synthesis; 1, 4-dihydropyridine ( amlodipine) , , --5- -2-( 2- - )-4-( 2- 2007 , )-6- -1, 4 - , 5-, , , ( Pfizer) 20 90 [1] , FDA [ 2] 1 : , , H