阿雷地平的合成  

Synthesis of Aranidipine

作　　者：李玲[1] 罗振福[1] 丁一[1] 

机构地区：[1]天津药物研究院,天津300193

出　　处：《中国医药工业杂志》2008年第1期6-8,共3页Chinese Journal of Pharmaceuticals

摘　　要：丙炔醇和乙二醇经加成后与双乙烯酮反应得乙酰乙酸2,2-亚乙二氧基丙酯,再经胺化、与2-(2-硝基亚苄基)-3-氧代丁酸甲酯缩合、水解得抗高血压药阿雷地平,总收率约为34%。Aranidipine was synthesized by the addition of propynol and ethylene glycol followed by reaction with ketene dimer to give 2,2-ethylenedioxypropyl acetoacetate, which was subjected to amination, condensation with 2-（2-nitrobenzylidene）-3-oxobutyric acid methyl ester and then hydrolysis with an overall yield of about 34 %.

关 键 词：阿雷地平 抗高血压药 钙拮抗剂 合成 

分 类 号：R972.4[医药卫生—药品]