Organocatalytic radical aminoacylation of alkenes forβ-aminoketone synthesis  

作　　者：Ayisenbati Jialingbieke Xinying Hu Zuquan Liu Xiyun Lin Yiwen Yin Jibin Li Yatian Huang Ding Du 

机构地区：[1]State Key Laboratory of Natural Medicines,School of Science,China Pharmaceutical University,Nanjing 210009,China

出　　处：《Science China Chemistry》2025年第3期1002-1008,共7页中国科学(化学英文版)

基　　金：supported by the the National Natural Science Foundation of China (22371297)。

摘　　要：An NHC organocatalytic radical aminoacylation of alkenes has been developed by using aldehydes as the acylating reagents and activated aryloxy-amides as the N-radical precursors,providing a new platform for modular access to highly functionalizedβ-aminoketones.The key to the success of this reaction relies on the single electron transfer(SET)event between the enolates of Breslow intermediates and carefully screened N-radical precursors,followed by a radical addition and radical-radical coupling relay process.The protocol features simple and readily available materials(abundant and feed-stock aldehydes and alkenes),mild reaction conditions(metal-,photo-and oxidant-free,in EA at room temperature),easily removable protecting group for late-stage functionalization.

关 键 词：difunctionalization of alkenes ORGANOCATALYSIS CARBENE radical relay AMINOACYLATION β-aminoketone synthesis 

分 类 号：TQ226.35[化学工程—有机化工]