利伐沙班中间体的合成工艺研究

Study on the synthetic technology of intermediate of rivaroxaban

本文以溴苯为起始原料,经Ullmann反应、N-酰基化、吗啉酮环合、芳环硝基化、芳硝基还原、2-噁唑烷酮环合共六步反应制得了利伐沙班的关键中间体,所得目标化合物经质谱、核磁共振氢谱确认,总收率达到44.50%。

Intermediate of rivaroxaban was synthesized from bromobenzene by Ullmann reaction,N-acetoxylation,cyclization of mor-pholin-3-one,nitration of arene, reduction and cyclization of 2-oxazolidone. The target compound was identified by MS and 1 H-NMR,and the overall yield was 44. 50%.