Neighboring group-directed asymmetric [2+2+2] cycloaddition to access C-N axially chiral indoles

A Rh-catalyzed neighboring group-directed asymmetric [2 + 2 + 2] cycloaddition of 1,6-diynes and ynamides to generate C-N axially chiral indole derivatives has been developed. The notable features of this method include 100% atom-economy, a wide substrate scope and excellent enantioselectivities by using the easily available chiral SEGPHOS ligands. A Rh-catalyzed neighboring group-directed asymmetric [2 + 2 + 2] cycloaddition of 1,6-diynes and ynamides to generate C-N axially chiral indole derivatives has been developed.