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.
Chemistry, University of Southampton, Highfield, Southampton, Hampshire SO17 1BJ, UK. dch2@soton.ac.uk.
Zeshan
Z
Yousuf
Andrew K
AK
Richards
Andrew N
AN
Dwyer
Bruno
B
Linclau
David C
DC
Harrowven
D015057:1-Naphthylamine / Q000737:chemistry*; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry*; D015394:Molecular Structure; D009284:Naphthols / Q000737:chemistry
D007211:Indoles; D009284:Naphthols; C046649:ropinirole; D015057:1-Naphthylamine