Synthesis of Fused-Ring Pyrrolizine Derivatives via a Copper-Catalyzed Radical Cascade Cyclization

Author:

Ding Dong1,Ji Ya-Fei2,Xu Xiao-Bo2,Hao Li-Qiang2,Liu Xian2,Wang Yang-Yang2,Yang Zhao-Zi-Yuan2,Yu Xiao2

Affiliation:

1. Fuan Pharmaceutical Group, Chongqing Bosen Pharmaceutical Co., Ltd.

2. Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education; School of Pharmacy, East China University of Science & Technology

Abstract

AbstractHerein, an atom-economic method for the synthesis of fused-ring pyrrolizine derivatives by a cycloaddition reaction of easily accessible N-substituted pyrrole-2-carboxaldehydes with N-substituted maleimides in the presence of di-tert-butyl peroxide has been successfully developed. A total of 23 compounds were obtained by using this method, with a maximum yield of 72%, providing a practical and efficient method for the synthesis of tricyclic pyrrolizine frameworks.

Funder

National Natural Science Foundation of China

Publisher

Georg Thieme Verlag KG

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