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We report that halogenophilic silver(I) triflate permits halogen exchange (halex) nucleophilic (18)F-fluorination of aryl-OCHFCl, -OCF2Br and -SCF2Br precursors under mild conditions. This Ag(I)-mediated process allows for the first time access to a range of (18)F-labeled aryl-OCHF2, -OCF3 and -SCF3 derivatives, inclusive of [(18)F]riluzole. The (18)F-labeling of these medicinally important motifs expands the radiochemical space available for PET applications.

Original publication

DOI

10.1002/anie.201504665

Type

Journal article

Journal

Angew Chem Int Ed Engl

Publication Date

17/08/2015

Volume

54

Pages

9991 - 9995

Keywords

[18F]fluoride, difluoromethyl ethers, halogen exchange, silver triflate, trifluoromethyl ethers, Fluorine Radioisotopes, Hydrocarbons, Fluorinated, Molecular Structure, Organometallic Compounds, Silver