Enantioselective Synthesis of Indole-Based Biaryl Atropisomers via Palladium-Catalyzed Dynamic Kinetic Intramolecular C–H Cyclization

Abstract

We report here a palladium-catalyzed enantioselective synthesis of indole-based atropisomers via an intramolecular dynamic kinetic C–H cyclization. The TADDOL-derived phosphoramidite ligand proves to be most efficient in this directing-group-free transformation, delivering products with up to 96:4 er. The thermal stability of the axial chirality of the atropisomers has also been investigated.