Attrition‐Enhanced Deracemization of the Antimalaria Drug Mefloquine. Issue 6 (21st December 2018)

• Record Type: Journal Article
• Authors: Engwerda, Anthonius H. J.; Maassen, Rick; Tinnemans, Paul; Meekes, Hugo; Rutjes, Floris P. J. T.; Vlieg, Elias
• Is Part Of: Angewandte Chemie international edition. Volume 58:Issue 6(2019)
• Page Start: 1670
• Page End: 1673
• Publication Date: 2018-12-21
• Subjects: chirality -- deracemization -- drug discovery -- medicinal chemistry -- synthetic methods; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201811289
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: Mefloquine is an important drug for prevention and treatment of malaria. It is commercially available as a racemic mixture, wherein only one enantiomer is active against malaria, while the other one causes severe psychotropic effects. By converting the drug into a compound that crystallizes as a racemizable racemic conglomerate, the deracemization of mefloquine into the desired enantiomer was achieved. Abstract : Grinding out side‐effects : By grinding of a suspension of crystals in combination with a racemization reaction, the initial racemic mixture of the anti‐malaria drug mefloquine is deracemized to deliver the desired enantiomer.