Enantioselective Synthesis of Indole-Derivated Axially Chiral Frameworks via Cp^XRh(III)-Catalyzed Domino Cyclization/C₃-Arylation of 2-Alkynylanilines with 1-Diazonaphthoquinones

We report herein a chiral (CpRh)-Rh-X(III)-catalyzed domino cyclization/C-3-arylation process using 2-alkynylanilines and 1-diazonaphthoquinones as viable substrates, delivering indole-based derivatives endowed with axial chirality. The method features high enantioselectivity, broad substrate scope, and robust functional group tolerance. Subsequent functionalization of the synthesized scaffolds underlines the practicality of this approach in the design of indole-derivated axially chiral frameworks, demonstrating its substantial promise in synthetic and medicinal chemistry applications.