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■ Ruthenium(II)-Catalyzed ortho Hydroxymethylation of 6-Arylpurines with Paraformaldehyde via Purine-Directed C-H Activation

Jiaqi Jiang, Junli Yang, Siqi Li, Yaxi Yang,* and Bing Zhou*

*State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China

Abstract

A Ru-catalyzed ortho C-H hydroxymethylation of 6-arylpurines has been developed. A wide range of functional groups were tolerated, providing the hydroxymethylated products in good or excellent yields using the readily available paraformaldehyde as a C1 synthon. Moreover, this protocol could be carried out in the presence of water and air, without stoichiometric undesirable waste under mild reaction conditions.