Palladium‐Catalyzed Synthesis of (Hetero)Aryl Alkyl Sulfones from (Hetero)Aryl Boronic Acids,Unactivated Alkyl Halides,and Potassium Metabisulfite |
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Authors: | Andre Shavnya Dr. Kevin D. Hesp Dr. Vincent Mascitti Dr. Aaron C. Smith |
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Affiliation: | Pfizer, Inc., Worldwide Medicinal Chemistry, Groton, CT 06340 (USA) |
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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. |
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Keywords: | alkylation boronic acids homogeneous catalysis palladium sulfones |
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