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.

• Zeshan Yousuf^a
• Andrew K. Richards^b
• Andrew N. Dwyer^c
• Bruno Linclau^a
• 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

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