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.

Keywords

Lactams - Amides - Arylation - Palladium - Catalysis - α-Arylation

Publikationsverlauf

Eingereicht: 18. November 2025

Angenommen nach Revision: 12. Dezember 2025

Accepted Manuscript online:
12. Dezember 2025

Artikel online veröffentlicht:
24. Dezember 2025

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