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Palladium‐Catalyzed Synthesis of (Hetero)Aryl Alkyl Sulfones from (Hetero)Aryl Boronic Acids,Unactivated Alkyl Halides,and Potassium Metabisulfite
Authors:Andre Shavnya  Dr. Kevin D. Hesp  Dr. Vincent Mascitti  Dr. Aaron C. Smith
Affiliation:Pfizer, Inc., Worldwide Medicinal Chemistry, Groton, CT 06340 (USA)
Abstract:A palladium‐catalyzed one‐step synthesis of (hetero)aryl alkyl sulfones from (hetero)arylboronic acids, potassium metabisulfite, and unactivated or activated alkylhalides is described. This transformation is of broad scope, occurs under mild conditions, and employs readily available reactants. A stoichiometric experiment has led to the isolation of a catalytically active dimeric palladium sulfinate complex, which was characterized by X‐ray diffraction analysis.
Keywords:alkylation  boronic acids  homogeneous catalysis  palladium  sulfones
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