抗组胺新药富马酸依美斯汀的合成

Synthesis of a new anti-histamine drugemedastine difumarate

目的研究抗组胺新药富马酸依美斯汀的合成。方法以邻苯二胺为起始原料 ,经酸化、缩合、氯代、取代及成盐 6步反应合成富马酸依美斯汀 (8)。结果与结论以总收率 10 %合成了富马酸依美斯汀 ,并改进了重要中间体 1 (2 乙氧乙基 ) 2 氯苯并咪唑 (5 )和依美斯汀 (7)

Aim To study on the synthesis of emedastine difumarate.Methods Emedastine difumarate was synthesized via six steps starting from o phenylenediamine.Results and Conclusions The target compound was identified through spectroscopic analysis in the overall yield of 10%.The preparative methods of the key immediate 1 (2 ethoxyethyl) 2 chlorobenzimidazole(5)and emedastine(7)are improved.