Ruthenium-catalysed decarboxylative unsymmetric dual ortho -/ meta -C-H bond functionalization of arenecarboxylic acids

Here, we describe a ruthenium-catalysed decarboxylative unsymmetric -C-H azaarylation/ -C-H alkylation a traceless directing group relay strategy. The installation of a 2-pyridyl functionality carboxyl directed -C-H activation is critical to promote decarboxylation and enable -C-H bond alkylation to streamline the synthesis of 4-azaaryl-benzo-fused five-membered heterocycles. This protocol is characterized by high regio- and chemoselectivity, broad substrate scopes, and good functional group tolerance under redox-neutral conditions.