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

Kaira Wu; Alfredo Fuentes-Gutierrez; Olivier Rene

doi:10.1055/a-2772-4605

Synlett, Inhaltsverzeichnis

Synlett
DOI: 10.1055/a-2772-4605

Letter

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

Autor*innen

Kaira Wu

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

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

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

Abstract

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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.

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