Palladium-catalysed ortho-acylation of 6-anilinopurines/purine nucleosides via C–H activation

Purinyl N1 directed ortho-acylation of 6-anilinopurines was achieved via C(sp2)–H bond activation in the presence of [Pd]-catalyst using aldehydes or α-oxocarboxylic acids as the acylating source. A wide variety of purine appended 2′-aminoacetophenones/benzophenones are isolated in good to excellent yields. These catalytic transformations are also successfully applied to 6-anilinopurine nucleosides.