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Synthesis of (+)-Mefloquine Hydrochloride
J. D. Knight, S. J. Sauer, D. M. Coltart*
Duke University, Durham, USA
19 August 2011 (online)
Racemic mefloquine hydrochloride (Lariam®) is used for the treatment and prevention of malaria. The (+)-enantiomer is slightly more active than the (-)-enantiomer and it displays reduced neurotoxicity. The key step in the synthesis depicted is the asymmetric Darzens reaction (A → C) involving a hydrazone chiral auxiliary.