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Synlett
DOI: 10.1055/a-2772-4605
Letter

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

Authors

  • Kaira Wu

    1   Global Discovery Chemistry, Novartis Institutes for BioMedical Research Inc, Emeryville, United States (Ringgold ID: RIN33413)

  • Alfredo Fuentes-Gutierrez

    1   Global Discovery Chemistry, Novartis Institutes for BioMedical Research Inc, Emeryville, United States (Ringgold ID: RIN33413)

  • Olivier Rene 

    2   Global Discovery Chemistry, Novartis Institutes for BioMedical Research Emeryville, Emeryville, United States (Ringgold ID: RIN98558)
Further Information
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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.



Publication History

Received: 18 November 2025

Accepted after revision: 12 December 2025

Accepted Manuscript online:
12 December 2025

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