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Synthesis of 2-Aminopyrroles Via Metal-Free Annulation of Ynamides with 2H-Azirines. 2022
Lianhong Jiao, and
Yanan Wang, and
Lixia Ding, and
Chaofeng Zhang, and
Xiao-Na Wang, and
Junbiao Chang
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.
A novel metal-free annulation of ynamides with 2H-azirines catalyzed by BF3·Et2O 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.
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