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An improved and scalable synthesis of zolpidem via a CuI/BINOL-mediated tandem reaction of imine and alkyne 期刊论文

编号：

2ddc1133-ed65-42c9-b6fd-41d086c226af
作者：

Zhang, Bingbing^[1];Shan, Guangsheng^[1];Ma, Qiaoning^[1];Xu, Qianqian^[1];Lei, Xinsheng(雷新胜)*^[1]
语种：

English
期刊：

HETEROCYCLIC COMMUNICATIONS ISSN：0793-0283 2017 年 23 卷 6 期 (445 - 448) ; DEC
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关键词：

copper heterocycles hypnotic tandem reaction zolpidem
摘要：

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 propio-lamide 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.
推荐引用方式
GB/T 7714：

Zhang Bingbing,Shan Guangsheng,Ma Qiaoning, et al. An improved and scalable synthesis of zolpidem via a CuI/BINOL-mediated tandem reaction of imine and alkyne [J].HETEROCYCLIC COMMUNICATIONS,2017,23(6):445-448.
APA：

Zhang Bingbing,Shan Guangsheng,Ma Qiaoning,Xu Qianqian,&Lei Xinsheng.(2017).An improved and scalable synthesis of zolpidem via a CuI/BINOL-mediated tandem reaction of imine and alkyne .HETEROCYCLIC COMMUNICATIONS,23(6):445-448.
MLA：

Zhang Bingbing, et al. "An improved and scalable synthesis of zolpidem via a CuI/BINOL-mediated tandem reaction of imine and alkyne" .HETEROCYCLIC COMMUNICATIONS 23,6(2017):445-448.

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