Organic Chemistry Portal



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

Mingyang Li, Ying Xie, Yong Ye*, Yong Zou, Huanfeng Jiang and Wei Zeng*

*School of Chemistry and Chemical Engineering, South China University of Technolgy, Guangzhou 510641, China, Email:,

M. Li, Y. Xie, Y. Ye, Y. Zou, H. Jiang, W. Zeng, Org. Lett., 2014, 16, 6232-6235.

DOI: 10.1021/ol503165b

see article for more reactions


Copper(I) catalysis enables a direct transannulation of N-heteroaryl aldehydes or ketones with alkylamines via Csp3-H amination in the presence of oxygen as the sole oxidant. This transformation provides a rapid and concise access to multifunctional imidazo[1,5-a]pyridines.

see article for more examples

Key Words

imidazo[1,5-a]pyridines, oxygen

ID: J54-Y2014