亚胺
化学
唑吡坦
产量(工程)
串联
组合化学
对映体
色谱法
有机化学
催化作用
药理学
医学
复合材料
冶金
材料科学
失眠症
作者
Bingbing Zhang,Guangsheng Shan,Qiaoning Ma,Qianqian Xu,Xinsheng Lei
出处
期刊:Heterocyclic Communications
[De Gruyter]
日期:2017-11-14
卷期号:23 (6): 445-448
被引量:5
摘要
Abstract An improved and scalable method for the synthesis of zolpidem ( 1 ), a hypnotic drug, was developed. A two-step sequence involving imine formation and subsequent tandem reaction between an imine and propiolamide in the presence of CuI/BINOL, an efficient promoter for the tandem reaction, is described. Zolpidem was efficiently prepared in a 54% isolated yield and the hemitartrate salt of zolpidem was produced in 37% yield by simple crystallization, without tedious column chromatography. The procedure can be scaled up to >10 g. The yield of 1 increased to 83% following isolation of the intermediate imine 5 .
科研通智能强力驱动
Strongly Powered by AbleSci AI