Literature DB >> 30508314

Attrition-Enhanced Deracemization of the Antimalaria Drug Mefloquine.

Anthonius H J Engwerda1, Rick Maassen1, Paul Tinnemans1, Hugo Meekes1, Floris P J T Rutjes1, Elias Vlieg1.   

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.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  chirality; deracemization; drug discovery; medicinal chemistry; synthetic methods

Mesh:

Substances:

Year:  2018        PMID: 30508314     DOI: 10.1002/anie.201811289

Source DB:  PubMed          Journal:  Angew Chem Int Ed Engl        ISSN: 1433-7851            Impact factor:   15.336


  4 in total

1.  Bis(mefloquinium) butane-dioate ethanol monosolvate: crystal structure and Hirshfeld surface analysis.

Authors:  James L Wardell; Mukesh M Jotani; Edward R T Tiekink
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2019-07-12

Review 2.  A Review of Modifications of Quinoline Antimalarials: Mefloquine and (hydroxy)Chloroquine.

Authors:  Dawid J Kucharski; Michalina K Jaszczak; Przemysław J Boratyński
Journal:  Molecules       Date:  2022-02-02       Impact factor: 4.411

3.  Influence of Ostwald's Rule of Stages in the Deracemization of a Compound Using a Racemic Resolving Agent.

Authors:  Tharit Lerdwiriyanupap; Giuseppe Belletti; Paul Tinnemans; Ruel Cedeno; Hugo Meekes; Elias Vlieg; Adrian E Flood
Journal:  Cryst Growth Des       Date:  2022-01-24       Impact factor: 4.076

4.  Photoracemization-Based Viedma Ripening of a BINOL Derivative.

Authors:  Giuseppe Belletti; Carola Tortora; Indradevi D Mellema; Paul Tinnemans; Hugo Meekes; Floris P J T Rutjes; Svetlana B Tsogoeva; Elias Vlieg
Journal:  Chemistry       Date:  2019-12-12       Impact factor: 5.236

  4 in total

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