Regio- and Enantioselective Construction of C-N Axially Chiral N-Triazolyl-α-carbolines via Pyridine-Directed Click Reaction.

Herein, a pyridine-directed click asymmetric [3 + 2] cyclization of internal alkynes has been disclosed, enabling efficient access to C-N axially chiral 5,5-membered heterobiaryl atropisomers. The reaction affords a class of structurally novel N-triazolyl-α-carboline derivatives in good yields, excellent regio- and enantioselectivities (up to 98% yield and 99% ee). Notably, this catalytic asymmetric protocol demonstrates remarkable efficiency and atom economy under mild conditions, along with broad substrate scope.