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

A copper(I)-catalyzed direct transannulation of N-heteroaryl aldehydes or ketones with alkylamines via C-sp(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.