Wenkai Li, Pengfei Jia, Ke Yang, Xiaoli Gu, Shanshan Shi, Yuhan Zhou, Jingping Qu, Baomin Wang
Co/salicyloxazoline (Salox)-catalyzed asymmetric C-H activation/spiro annulation is reported for the synthesis of spirocyclic γ-lactams with dual N-N axial and spiro-central chirality. Through an enantioselective desymmetrization protocol of the prochiral maleimide, products are obtained in yields of 34-62% with up to 95% ee and >20:1 dr. Axial chirality established during C-H activation directs subsequent enantioselective spiro-center formation. This protocol accommodates bioactive scaffolds, providing streamlined access to complex chiral N-heterocycles.