3-Amino-1-methyl-1 H-pyridin-2-one-Directed Pd Catalysis: C(sp)-H Activated Diverse Arylation Reaction.

A new bidentate directing group, 3-amino-1-methyl-1 H-pyridin-2-one, is introduced to achieve a powerful Pd metallacycle for selective γ-C(sp)-H activation and arylation of aromatic and aliphatic carboxylic acid derivatives. The versatility of the directing group is validated for remote arylation of β-C(sp)-H, β-C(sp)-H, and γ-C(sp)-H to achieve therapeutically important 2-pyridone analogues and arylated acid synthons. The traceless removal of the directing group to retrieve the directing element and carboxylic acids makes this method more interesting.