Enantioselective Copper‐Catalyzed Alkylation of Quinoline <i>N</i>‐Oxides with Vinylarenes

Abstract

An asymmetric copper-catalyzed alkylation of quinoline N-oxides with chiral Cu-alkyl species, generated by migratory insertion of a vinylarene into a chiral Cu-H complex, is reported. A variety of quinoline N-oxides and vinylarenes underwent this Cu-catalyzed enantioselective alkylation reaction, affording the corresponding chiral alkylated N-heteroarenes in high yield with high-to-excellent enantioselectivity. This enantioselective protocol represents the first general and practical approach to access a wide range of chiral alkylated quinolines.