Ligand‐Promoted meta‐C−H Functionalization of Benzylamines

Abstract Meta‐C−H functionalization of benzylamines has been developed using a Pd II /transient mediator strategy. Using 2‐pyridone ligands and 2‐carbomethoxynorbornene (NBE‐CO 2 Me) as the mediator, arylation, amination, and chlorination of benzylamines are realized. This protocol features a broad substrate scope and is compatible with heterocylic coupling partners. Moreover, the loading of the Pd can be lowered to 2.5 mol % by using the optimal ligand.