Metal-Free Approach to Zolpidem, Alpidem and their Analogues via Amination of Dibromoalkenes Derived from Imidazopyridine and Imidazothiazole
作者:Vasiliy M. Muzalevskiy、Zoia A. Sizova、Alexey V. Shastin、Valentine G. Nenajdenko
DOI:10.1002/ejoc.201900279
日期:2019.7.7
Zolpidem, Alpidem and their analogues was elaborated. A set of previously unknown dibromoalkenes derived from imidazopyridine and imidazothiazole was prepared using Wittig olefination of the corresponding aldehydes by CBr4‐PPh3 system. Amination of dibromoalkenes with different primary and secondary amines in the presence of water led directly to target drugs and their analogues in up to 95 % yield.
阐述了一种新的两步法制备唑吡坦,阿吡培南及其类似物。使用CBr 4 -PPh 3体系对相应的醛进行Wittig烯化反应,制得了一组由咪唑并吡啶和咪唑并噻唑衍生的未知二溴代烯烃。在水的存在下,用不同的伯胺和仲胺对二溴烯烃进行胺化可直接导致目标药物及其类似物的产率高达95%。