Jiao Lianhong, Wang Yanan, Ding Lixia, Zhang Chaofeng, Wang Xiao-Na, Chang Junbiao
Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, P. R. China.
J Org Chem. 2022 Nov 18;87(22):15564-15570. doi: 10.1021/acs.joc.2c02103. Epub 2022 Nov 4.
A novel metal-free annulation of ynamides with 2-azirines catalyzed by BF·EtO is described, leading to the construction of polysubstituted 2-aminopyrroles in a facile, flexible, and atom-economical way. This synthetic strategy proceeds with efficiency, broad substrate scope, and short reaction time under mild reaction conditions. Furthermore, the obtained annulation products could be modified to generate diverse 2-iminopyrrole frameworks in high yields.
描述了一种由BF·EtO催化的新型无金属的烯酰胺与2-氮杂环丙烯的环化反应，该反应以简便、灵活且原子经济的方式构建多取代的2-氨基吡咯。这种合成策略在温和的反应条件下具有高效性、广泛的底物范围和较短的反应时间。此外，所得到的环化产物可以进行修饰，以高产率生成多种2-亚氨基吡咯骨架。
