硝酸依柏康唑的合成新方法  

Novel Synthesis of Eberconazole Nitrate

作　　者：程炜[1] 汤俊梅[1] 顾准[1] CHENG Wei TANG Jun-mei GU Zhun(Department of Biological and Chemical Engineering, Suzhou Chien-Shiung Institute of Technology, Taieang 215411, China)

机构地区：[1]苏州健雄职业技术学院生物与化学工程系,江苏太仓215411

出　　处：《化学试剂》2017年第10期1129-1131,共3页Chemical Reagents

基　　金：江苏省高校"青蓝工程"资助项目;太仓市科学技术局项目(TC2014GY19)

摘　　要：标题化合物是一种外用广谱抗真菌感染药物,以邻苯二甲酸酐和3,5-二氯苯乙酸为原料,首先经缩合、催化加氢、环合3步反应制备得到关键中间体2,4-二氯-10,11-二氢-5H-二苯并[a,d]环庚烯-5-酮,然后经还原、氯化、N-烃基化、成盐等4步反应制备得到。该合成方法缩短了标题化合物的合成路线,提高了总收率,不产生有机磷废弃物,更适于工业化生产。Eberconazole nitrate is an external used broad-spectrum antifungal drug.In this work,the key intermediate 2,4-dichloro-10,11-dihydro-5H-dibenzo[a,d] cyclohepten-5-one was synthesized by condensation,catalytic hydrogenation,cyclization from phthalic anhydride and 3,5-dichlorophenylacetate.Then,the eberconazole nitrate was synthesized by the key intermediate via reduction,chlorination,N-alkylation and salification.The method is suitable for large-scale production due to shorter synthetic route,improved yield and no organic phosphorus waste.

关 键 词：硝酸依柏康唑 抗真菌感染 合成方法 

分 类 号：R914.5[医药卫生—药物化学]