Copper-Catalyzed C(sp3 )-Amination of Ketone-Derived Dihydroquinazolinones 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.