The development of a short route to the API ropinirole hydrochloride

    • Zeshan Yousufa
    • Andrew K. Richardsb
    • Andrew N. Dwyerc
    • Bruno Linclaua
    • David C. Harrowven* a
    • a Chemistry, University of Southampton, Highfield, Southampton, UK
    • b GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, UK
    • c Formally at GlaxoSmithKline Innovation and Sustainable Manufacturing COE, Worthing, UK
    The development of a short route to the API ropinirole hydrochloride

    A four-step, three-stage synthesis of the API ropinirole hydrochloride has been developed from a commercially available naphthalene derivative. The new route has half the step-count and twice the overall yield of the current manufacturing process. Key features of the synthesis are a regioselective Birch reduction and an ozonolysis with concomitant ring closure to induce the required ring contraction.

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