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Solvent- and Catalyst-Free Huisgen Cycloaddition to Rufinamide in Flow with a Greener, Less Expensive Dipolarophile

Authors

  • Svetlana Borukhova,

    1. Department of Chemical Engineering and Chemistry, Micro Flow Chemistry and Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612AZ, Eindhoven (The Netherlands)
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  • Dr. Timothy Noël,

    Corresponding author
    1. Department of Chemical Engineering and Chemistry, Micro Flow Chemistry and Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612AZ, Eindhoven (The Netherlands)
    • Department of Chemical Engineering and Chemistry, Micro Flow Chemistry and Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612AZ, Eindhoven (The Netherlands)

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  • Bert Metten,

    1. S.A. Ajinomoto OmniChem N.V. Cooppallaan 91, 9230 Wetteren (Belgium)
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  • Eric de Vos,

    1. S.A. Ajinomoto OmniChem N.V. Cooppallaan 91, 9230 Wetteren (Belgium)
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  • Prof. Dr. Volker Hessel

    Corresponding author
    1. Department of Chemical Engineering and Chemistry, Micro Flow Chemistry and Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612AZ, Eindhoven (The Netherlands)
    • Department of Chemical Engineering and Chemistry, Micro Flow Chemistry and Process Technology, Eindhoven University of Technology, Den Dolech 2, 5612AZ, Eindhoven (The Netherlands)

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Abstract

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Give it a flow: A continuous-flow process for the synthesis of a 1,2,3-triazole precursor of Rufinamide has been developed. The protocol involves a solvent- and catalyst-free operation and utilizes reaction temperatures above the melting point of the target product to prevent microreactor clogging, resulting in a decrease of the operating time from hours to minutes.

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