Nickel-catalyzed sp2 C–H bonds arylation of N-aromatic heterocycles with Grignard reagents at room temperature

Abstract

A novel protocol for nickel-catalyzed direct sp² C–H bond arylation of purines has been developed. This new reaction proceeded efficiently at room temperature using Grignard reagent as the coupling partner within 5 hours in good to high yields. This approach provides a new access to a variety of C8-arylpurines which are potentially of great importance in medicinal chemistry.