Asymmetric Synthesis of Hydroquinolines with α,α‐Disubstitution through Organocatalyzed Kinetic Resolution

The first kinetic resolution of hydroquinoline derivatives with α,α-disubstitution was realized through organocatalyzed asymmetric remote aminations with azodicarboxylates, which represents a powerful protocol for asymmetric synthesis of N-heterocycles with α-quaternary stereocenters. Mechanistic studies elucidate the reaction mechanisms and highlighted the role of attractive non-covalent interactions between the substrate and catalyst.