盐酸莫雷西嗪的合成

Synthesis of moracizine hydrochloride

目的:合成抗心律失常药盐酸莫雷西嗪。方法:以3-溴硝基苯、乙酰苯胺为原料经烃化、水解反应得3-硝基二苯胺,经硫化亚铁-氯化铵-甲醇-水体系还原得3-氨基二苯胺,再经酰化、环合、烃化和成盐反应得盐酸莫雷西嗪。结果:合成了盐酸莫雷西嗪,9步反应总收率为35．8%。目标产物的结构经核磁共振氢谱、质谱确证。结论:本合成方法原料易得,操作简单,收率较高,适合大规模制备。

Objective： To synthesize antiarrythmic drug moracizine hydrouhloride. Methods： Starting from 3-bromonitrobenzene and acetanilide, the intermediate 3-nitrodiphenyiamine was obtained via alkylation and hydrolysis. Subsequently, the target compound was synthesized via several chemical reactions including reduction, acylation, cyclization, alkylation and saltization. Results： The total yield of moracizine hydrochloride was 35.8% , and the structure was verified by ^1H-NMR and MS. Conclusion： An easily manipulated synthetic procedure of moracizine hydrochloride was achieved for further pilot manufacture.