Chiral Spiro Oxazoline Ligands for Cu-Catalyzed Asymmetric Oxidative Coupling

Chiral spiro ligands constitute privileged architectures that have enabled remarkable advances in asymmetric catalysis. Despite their widespread utility, non-C₂-symmetric variants remain significantly underdeveloped, limiting access to dissymmetric chiral environments with unique stereochemical control elements. Herein, we disclose the strategic design of a novel class of spiro oxazoline ligands featuring a non-C₂-symmetric aza-angular framework that integrates conformational rigidity with a tunable chiral pocket. The synthetic utility of this bidentate N,N-ligand platform is demonstrated through Cu-catalyzed asymmetric oxidative coupling of 2-naphthols, which proceeds under mild conditions to furnish enantioenriched BINOL derivatives in high yields with up to 94% ee.