Stereospecific Copper-Catalyzed Domino Ring Opening and sp3 C–H Functionalization of Activated Aziridines with N‑Alkylanilines

Copper efficiently catalyzed nucleophilic ring opening, sp3 C–H functionalization, and C–N bond formation in the presence of tert-butyl hydroperoxide to afford functionalized imidazolidines starting from N-sulfonylaziridines and N-alkylanilines. The products were obtained in high optical purities (95 → 99% ee) with excellent functional group tolerance.