Enantioselective Assembly of Planar-Chiral and Axial-Planar-Chiral Macrocycles <i>via De Novo</i> Isoquinolinone Formation

A mild cobalt/salicyloxazoline (Salox)-catalyzed intramolecular C-H macrocyclization is reported. This method enables the enantioselective synthesis of planar-chiral macrocycles as well as scaffolds integrating planar and axial chirality. The reaction proceeds under mild conditions, shows broad substrate scope, and delivers products in yields of 42% to 73% with excellent enantioselectivities (up to 99% ee). This work establishes a versatile platform for constructing constrained, three-dimensional macrocyclic architectures.