Cobalt-Catalyzed Enantioselective and Diasterodivergent Con-struction of Distal Chiral C-N Diaxes

Herein, we report an efficient method for the synthesis of atropisomers with distal 1,3–C–N diaxes using the co-balt/Salox system via C–H and N–H annulation with benzamide and sterically hindered alkynes. This one-step, step-economical process operates at room temperature with oxygen from air as the sole oxidant, removing the need for metal oxidants, photocatalysts, or electricity. The reaction is compatible with a broad range of arylamides and alkynes, providing high yields and excellent enantioselectivity (up to >99% ee). Experimental and DFT studies indicate that the migratory insertion is the rate-determining step, while C–H activation is the enantio-determining step.