4.8 Article

Mild Pd-Catalyzed N-Arylation of Methanesulfonamide and Related Nucleophiles: Avoiding Potentially Genotoxic Reagents and Byproducts

Journal

ORGANIC LETTERS
Volume 13, Issue 10, Pages 2564-2567

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol200660s

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Funding

  1. Lilly Research Laboratories

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A convenient, general, and high yielding Pd-catalyzed cross-coupling of methanesulfonamide with aryl bromides and chlorides Is reported. The use of this method eliminates concern over genotoxic impurities that can arise when an aniline is reacted with methanesulfonyl chloride. The application of this method to the synthesis of dofetilide is also reported.

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