Journal
TETRAHEDRON
Volume 71, Issue 19, Pages 2906-2913Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2015.03.061
Keywords
Trifluoromethylation; Pyrone; Pyridone; Quinolone; Methyl fluorosulfonyldifluoroacetate; Heteroaromatic
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Funding
- Irish Research Council for Science, Engineering and Technology (IRCSET)
- Pfizer Process Development Centre, Cork
- Science Foundation Ireland [SFI/12/IP/1315, SFI/12/RC/2275]
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2-Pyrones, pyridones and quinolones represent classes of molecules with remarkable and diverse biological activity. The introduction of a trifluoromethyl group to a molecule can have dramatic and beneficial effects in terms of lipophilicity and bioavailability. Herein we report a route to afford a library of novel trifluoromethylated 2-pyrones, 2-pyridones and a 2-quinolone in moderate to good yield using methyl fluorosulfonyldifluoroacetate as the trifluoromethylating agent. (C) 2015 Published by Elsevier Ltd.
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