Rhodium(III)-catalyzed regioselective oxidative annulation of anilines and allylbenzenes via C(sp3)–H/C(sp2)–H bond cleavage

Described herein is the merging of allylic C(sp3)–H activation and directed C(sp2)–H activation into a single approach for discovering unprecedented chemical transformations. As a proof-of-concept, we disclose for the first time the rhodium-catalyzed regioselective oxidative annulation of anilines with allylbenzenes to deliver a variety of indoles. In this work, the C3 and C2 positions of the allylic segment are set to construct C–N and C–C bonds, respectively.