A direct metal-free C2–H functionalization of quinoline N-oxides: a highly selective amination and alkylation strategy towards 2-substituted quinolines

Abstract

An efficient one-pot methodology for C2-selective amination and alkylation of quinoline N-oxides towards 2-substituted quinolines was developed, via the reaction of various quinoline N-oxides with ammonia, a large variety of primary and secondary amines, as well as active methylene compounds in the presence of diethyl H-phosphonate and K₂CO₃ under metal free conditions at room temperature.