Trapped in misbelief for almost 40 years: selective synthesis of the four stereoisomers of mefloquine

…, M Müller, UM Reinscheid, C Griesinger…

Index: Schuetzenmeister, Nina; Mueller, Michael; Reinscheid, Uwe M.; Griesinger, Christian; Leonov, Andrei Chemistry - A European Journal, 2013 , vol. 19, # 51 p. 17584 - 17588

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Citation Number: 9

Abstract

Abstract Here we report the synthesis of all four stereoisomers of mefloquine. Mefloquine (Lariam) is an important anti-malaria drug that is applied as a racemate of the erythro form. However, the (−)-isomer induces psychosis, while the (+)-enantiomer does not have this undesired side effect. There are six syntheses of which five lead to the wrong enantiomer without the authors of these syntheses noting that they had synthesized the wrong ...