Other Publication Details
Mandatory Fields
Reviews
Clarke, SL;McGlacken, GP
2017
January
Methyl fluorosulfonyldifluoroacetate (MFSDA): An Underutilised Reagent for Trifluoromethylation
Validated
1
WOS: 40 ()
Optional Fields
RAY PHOTOELECTRON-SPECTROSCOPY HIGHLY-ELECTRON-DEFICIENT MEDICINAL CHEMISTRY REGIOSELECTIVE TRIFLUOROMETHYLATION DIFLUOROCARBENE PRECURSORS BIOLOGICAL-ACTIVITY EFFICIENT SYNTHESIS COUPLING REACTIONS FACILE SYNTHESIS ORGANIC HALIDES
The introduction of fluorine groups to pharmaceutical compounds can have a dramatic effect on the lipophilicity and metabolic stability of the molecule in vivo. Around 20% of drugs contain at least one fluorine atom. The trifluoromethyl group is known to have beneficial effects and can dramatically affect the biological activity when substituted for a methyl group, for example. In any case, the direct and late-stage introduction of a trifluoro-methyl group is a powerful transformation in the tool box of the medicinal chemist. The use of methyl fluorosulfonyldifluoroacetate (MFSDA) as a relatively inexpensive reagent for trifluoromethylation was first reported in 1989; however, in our opinion it has been somewhat underutilised. Herein, a comprehensive review of trifluoromethylation using MFSDA is reported, which we hope will further expose readers to this useful reagent.
WEINHEIM
WILEY-V C H VERLAG GMBH
0947-6539
1219
1230
10.1002/chem.201602511
Grant Details