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Paper | Regular issue | Vol 100, No. 6, 2020, pp.934-945
Published online, 13th May, 2020
DOI: 10.3987/COM-20-14258
Ruthenium(II)-Catalyzed Regioselective C-H Hydroxymethylation of N-Aryl-azaindoles with Paraformaldehyde

Siqi Li, Yang Yu,* Yaxi Yang, and Bing Zhou*

*Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, PR, China

Abstract

A facile synthesis of hydroxymethylated N-aryl-azaindoles was developed via a Ru(II)-catalyzed regioselective C-H addition to paraformaldehyde. The reaction is compatible with air, shows high functional group tolerance and regioselectivity, and is an environmentally benign method without any undesired byproduct.