硝酸依柏康唑的合成新方法

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。

Novel Synthesis of Eberconazole Nitrate

Eberconazole nitrate is an external used broad-spectrum antifungal drug.In this work,the key intermediate 2,4-dichloro-10,11-dihydro-5H-dibenzoa,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.