抗真菌药阿莫罗芬的合成  

Synthesis of Antimycotic Agent Amorolfine

作　　者：冯志祥[1] 张万年[1] 周有骏[1] 陈卫平[1] 朱驹[1] 

机构地区：[1]第二军医大学药学院,上海200433

出　　处：《中国药物化学杂志》2000年第1期64-65,共2页Chinese Journal of Medicinal Chemistry

基　　金：军队"九五"重点课题!No .96z0 30

摘　　要：以叔戊基苯为原料 ,经羟甲基化、溴代 ,生成 4 溴甲基叔戊基苯 (2 ) ,再与甲基丙二酸二乙酯缩合 ,水解 ,脱羧 ,制得关键中间体 2 甲基 3 (4 叔戊基苯基 )丙酸 (3) ,与顺 2 ,6 二甲基吗啉成酰胺 ,还原得到阿莫罗芬 .By hydroxymethylation and bromination from tert pentylphene,4 bromomethyl tert pentylphene was prepared,which was coupled with methyl malonic ester,hydrolysized and decarboxylated to afford the key intermediate 2 methyl 3 (4 tert pentylphenyl)propionic acid,this intermediate was amidated with cis 2 ,6 dimethylmorpholine and reduced to synthesized amorolfine.The overall yield was 55 4%.

关 键 词：阿莫罗芬 合成 抗真菌活性 

分 类 号：R914[医药卫生—药物化学]