NiH-Catalyzed Regioselective Hydroamidation of Unactivated Alkenes with Dioxazolones

A nickel-catalyzed intermolecular hydroamidation of alkenes with dioxazolones has been developed, enabling the efficient synthesis of valuable β- and γ-amino acid derivatives. The presence of a directing group is pivotal to the reaction's success. This methodology is characterized by mild reaction conditions, high regioselectivity, with excellent functional group tolerance, and the elimination of additional ligand requirements. The practical applicability of this approach was further validated through large-scale reactions and the late-stage functionalization of pharmaceutical molecules.