Nickel-catalyzed decarboxylative acylation of heteroarenes by sp2 C-H functionalization

Chemistry. 2014 Jun 10;20(24):7241-4. doi: 10.1002/chem.201402516. Epub 2014 May 13.

Abstract

Nickel-catalyzed ligand-free decarboxylative cross-coupling of azole derivatives with α-oxoglyoxylic acids has been developed. This work represents the first example of decarboxylative cross-coupling reactions, in a C-H bond functionalization manner, through nickel catalysis, and tolerates various functional groups. Additionally, this approach provides an efficient access to azole ketones, an important structural motif in many medicinal compounds with a broad range of biological activities.

Keywords: acylation; decarboxylation; heteroarenes; nickel; sp2 CH bond functionalization.