抗真菌药阿莫罗芬中间体的合成研究

Improved Synthesis of the Intermediate of Antimycotic Agent Amorolfine

目的:合成阿莫罗芬重要中间体。方法:以苯为原料,经Friedel-Crafts烷基化和酰化制备叔戊基苯丙酮,再由叔戊基苯丙酮与甲醛,顺-2,6-二甲基吗啉通过Mannish反应制得顺-4-[2-甲基-3-氧代-3-(对叔戊基苯基)丙基]-2,6二甲基吗啉这一重要中间体。结果:总收率32.16%。结论:目标化合物是合成阿莫罗芬的理想前体。

Objective： To afford the key intermediate of Amorolfine. Method ： By Friedel-Crafts alkylation and aeylation from benzene ,4-tert-pentyl phenylpropanone was prepared ,which was trippled with formaldehyde and eis-2,6- dimethy-morpholine to make mannish reaction to afford the key intermediate eis4-12-methyl-3-oxygenie-3-（4-tert-pentyl-phenyl） propionie]-2,6-dimethy- mor pholine. Result： Total yield was 32.16%. Conclusion： Target compound is a suitable intermediate of synthese of Amorolfine.