Cu(I)-Catalyzed Transannulation of <i>N</i>-Heteroaryl Aldehydes or Ketones with Alkylamines via C(sp³)–H Amination

Abstract

A copper(I)-catalyzed direct transannulation of N-heteroaryl aldehydes or ketones with alkylamines via Csp(3)-H amination has been achieved using molecular oxygen as a sole oxidant. N-Heteroarenes are employed as the amine source. This transformation provides a rapid and concise access to multifunctional imidazo[1,5-a]pyridines.