Rhodium-Catalyzed [3 + 2] Annulation of 2-Benzylquinazolinones with Ketones for the Synthesis of Diversely Functionalized Pyrrolo[2,1-b]quinazolinones.

A Rh(III)-catalyzed [3 + 2] annulation strategy is developed for the synthesis of pyrrolo[2,1-b]quinazolinones from readily available 2-benzylquinazolinones and ketones via sp3 C-H activation. This protocol enables the efficient introduction of diverse functional groups such as aryl, polyaromatic, heteroaromatic, and alkyl substituents onto the bioactive pyrrolo[2,1-b]quinazolinone frameworks depending on the ketone employed.