摘要
以6-溴-4-((4-(4-(叔丁氧基羰基)哌嗪-1-基)-3-(三氟甲基)苯基)氨基)喹啉-3-羧酸乙酯为原料,经偶联、还原、氧化、成环、脱保护和酰基化六步反应以40%的总收率合成了Torin1,其结构经1H NMR确认无误。与文献报道方法相比较,新线路减少了副反应的发生,简化工艺操作,降低的分离难度,提高了收率和产品纯度,适用于低成本规模化生产。
Started from ethyl 6-bromo-4- （ （4- （4- （tert-butoxycarbonyl） piperazin- 1 -yl） - 3 - （trifluoromethyl） phenyl） amino）quinoline-3-carboxylate, Torinl was synthesized by six steps of reaction included coupling, reduction, oxidation, ring, deprotected and acylated. Structure of products was characterized by I H NMR. Compared with reported methods, this route suppressed side reactions, simplified reaction and isolation process, and increased yield and purity. It was suitable for industrialized production.
出处
《广州化工》
CAS
2017年第3期25-26,59,共3页
GuangZhou Chemical Industry
基金
烟台大学博士科研启动资金项目(HY07B30)
