Direct C–H Functionalization of Pyridine via a Transient Activator Strategy: Synthesis of 2,6-Diarylpyridines

Abstract

A Pd-catalyzed highly selective direct diarylation of pyridines has been developed using a transient activator strategy. Both (MeO)₂SO₂ and Cu₂O are required for this transformation. The in situ generated N-methylpyridinium salt can be arylated at both 2- and 6-positions under the cooperative Pd/Cu catalysis. A subsequent N-demethylation then gives the 2,6-diarylpyridines. This protocol provides a novel synthetic route for the symmetric 2,6-diarylpyridines.