Palladium-Catalyzed α-Arylation of Boc-Protected Lactams Using 2,2,6,6-Tetramethylpiperidine·ZnCl·LiCl

Abstract We report general conditions for the palladium-catalyzed α-arylation of Boc-protected lactams using TMP·ZnCl·LiCl as a base, eliminating the need for preformed zinc amide enolates. The method is compatible with various 5- and 6-membered lactams and a broad range of aryl bromides. These operationally simple conditions enable efficient access to α-arylated lactams, streamlining SAR exploration in medicinal chemistry.