Alkoxy Radical‐Triggered 1,1,2‐Trifunctionalization of Unactivated Alkenes towards N,O‐Spiroaminals

Comprehensive Summary N,O‐Spiroaminals have potential biological activities and abilities to modulate the physicochemical and pharmacokinetic properties of drug molecules. However, effective catalytic methods for the efficient construction of N,O‐spiroaminals are still limited to date. Herein, we report a novel 1,1,2‐trifunctionalization of unactivated alkenes to rapidly and efficiently obtain a diverse array of architecturally intriguing N,O‐spiroaminals. This methodology exhibits broad substrate scope, good functional group compatibility, and potential synthetic utility by a scale‐up reaction, diverse product derivatizations and late‐stage functionalization of complex biorelevant molecule. Notably, this transformation selectively allows for the formation of three new chemical bonds (C–O, C–C, and C–N) and one spiro quaternary carbon center across C‐C double bonds.