In Situ Preparation and Consumption of O-Mesitylsulfonylhydroxylamine (MSH) in Continuous Flow for the Amination of Pyridines

    Cara E. Brocklehurst*, Guido Koch, Stephanie Rothe-Pöllet, Luigi La Vecchia

    • Synthesis and Technologies, Global Discovery Chemistry, Novartis Institutes for Biomedical Research, Klybeckstrasse 141, 4057 Basel, Switzerland

    The paper demonstrates a safe method in which highly unstable O-mesitylsulfonylhydroxylamine (MSH) can be prepared and consumed in continuous flow. MSH was prepared in situ and used for the flow amination of a range of pyridines, which were subsequently transformed into useful pyrazolopyridine building blocks.

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