Reductive N-methylation of quinolines with paraformaldehyde and H2 for sustainable synthesis of N-methyl tetrahydroquinolines

Abstract

A new and straightforward method was developed for the synthesis of N-methyl-1,2,3,4-tetrahydroquinolines by one-pot reductive N-methylation of quinolines with paraformaldehyde and H₂ over Pd/C catalyst. A series of functional MTHQs, including (±)-galipinine and (±)-angustrureine were successfully synthesized in good to excellent yields by applying this simple catalyst system.