Assignment of Absolute Configuration to Enantiomers of Anti-Alzheimer Drug Candidate Blarcamesine

Authors

  • Zsuzsanna Szokol
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • Károly Lozsi
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • Attila Virág
    Affiliation
    Directorate of Finished Product Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • András Dancsó
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • László Szlávik
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • Gyula Simig
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
  • Balázs Volk
    Affiliation
    Directorate of Drug Substance Development, Egis Pharmaceuticals Plc., H-1475 Budapest, P. O. B. 100, Hungary
https://doi.org/10.3311/PPch.20662

Abstract

Blarcamesine is a promising investigational drug for the treatment of Alzheimer's disease. The international nonproprietary name blarcamesine refers to a racemic compound, although it seems likely that it will be marketed in an enantiopure form. A resolution process has been described in the literature, but the absolute configurations of the enantiomers have not yet been disclosed. In the present study, crystals of (R)-(-)- and (S)-(+)-mandelate salts of (+)- and (-)-blarcamesine and also that of (R)-(+)-blarcamesine itself, suitable for single-crystal X-ray diffraction measurement were prepared and the absolute configurations of (+)- and (-)-blarcamesine have been determined.

Keywords:

blarcamesine, resolution, crystallization, absolute configuration, single-crystal X-ray diffraction

Citation data from Crossref and Scopus

Published Online

2022-10-03

How to Cite

Szokol, Z., Lozsi, K., Virág, A., Dancsó, A., Szlávik, L., Simig, G. “Assignment of Absolute Configuration to Enantiomers of Anti-Alzheimer Drug Candidate Blarcamesine”, Periodica Polytechnica Chemical Engineering, 66(4), pp. 536–540, 2022. https://doi.org/10.3311/PPch.20662

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