Palladium-Catalyzed α-arylation improves lactam synthesis, streamlining exploration in medicinal chemistry.
We report general conditions for the palladium-catalyzed α-arylation of Boc-protected lactams using TMP·ZnCl·LiCl as 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.
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Wu et al. (2025) studied this question.
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