Copper-Catalyzed Formal C-N Bond Cleavage of Aromatic Methylamines: Assembly of Pyridine Derivatives

An efficient copper-catalyzed C-N bond cleavage of aromatic methylamines was developed to construct pyridine derivatives. With neat conditions and facile operation, the fragment-assembling strategy. affords a broad. range Of 2,4,6-trisubstituted pyridines in up to 95% yield from simple and readily available starting materials. Interestingly, when pyridin-2-yl methylamine Was employed as the substrate, alpha-alkylation reaction of ketones readily occurred to give beta-(pyridin-2-yl) ketones instead of the 2,4,6-trisubstituted pyridines.