Copper-Catalyzed Electrophilic Amination of Arylboronic Acids with Anthranils: An Access to <i>N</i>-Aryl-2-aminophenones
Yang Gao, Simin Yang, Yibiao Li, Yanping Huo, Zongyi Huang, Zumin Chen, Xiao‐Qiang Hu
Abstract
An efficient copper-catalyzed electrophilic amination strategy has been established for the rapid synthesis of N-aryl-2-aminophenones from readily available arylboronic acids/esters and anthranils. This protocol features good functional group tolerance, broad substrate scope, and operational simplicity. Moreover, a tandem C–H borylation and C–N coupling protocol has also been developed to transform simple arenes to the valuable N-aryl-2-aminophenones in one pot. Additionally, the synthetic potential of this methodology is further demonstrated by the synthesis of various useful N-heterocycles and derivatives.
Topics & Concepts
Electrophilic aminationAminationArylElectrophileCatalysisChemistryCopperOrganic chemistryMedicinal chemistryCombinatorial chemistryAlkylCatalytic C–H Functionalization MethodsCatalytic Cross-Coupling ReactionsRadical Photochemical Reactions