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Thursday, September 29, 2011

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


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.

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

Chem. Commun., 2011, 47, 11140-11142

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