Issue 20, 2009

Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine

Abstract

Two novel SF5 analogs of the antimalarial agent mefloquine were synthesized in 5 steps and 10–23% overall yields and found to have improved activity and selectivity against malaria parasites. This work also represents the first report of SF5-substituted quinolines.

Graphical abstract: Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine

Supplementary files

Article information

Article type
Communication
Submitted
12 Jun 2009
Accepted
27 Jul 2009
First published
07 Aug 2009

Org. Biomol. Chem., 2009,7, 4163-4165

Synthesis and biological evaluation of the first pentafluorosulfanyl analogs of mefloquine

P. Wipf, T. Mo, S. J. Geib, D. Caridha, G. S. Dow, L. Gerena, N. Roncal and E. E. Milner, Org. Biomol. Chem., 2009, 7, 4163 DOI: 10.1039/B911483A

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