Enantioselective Synthesis of N-Substituted Indoles with α,β-Stereocenters via Sequential Aza-Piancatelli/Cyclization Reactions

A sequence of catalytic asymmetric aza-Piancatelli rearrangement and Pd-catalyzed cyclization has been developed to construct chiral N-substituted indoles featuring α,β-consecutive stereocenters. This indole framework, bearing α,β-chiral centers, is a prevalent structural motif in natural products and biologically active molecules, yet catalytic enantioselective methods for its preparation remain scarce. This protocol offers efficient access to a diverse array of N-substituted indole derivatives with α,β-consecutive stereocenters, achieving high yields and excellent enantioselectivities.