Copper-Catalyzed C(sp3)-Amination of Ketone-Derived Dihydro-quinazolinones by Aromatization-Driven C-C Bond Scission

Herein, we describe the development of a copper-catalyzed C(sp³)-amination of proaromatic dihydroquinazolinones derived from ketones. The reaction is enabled by the intermediacy of open-shell species arising from homolytic C−C bond-cleavage driven by aromatization. The protocol is characterized by its operational simplicity and generality, including chemical diversification of advanced intermediates.