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[ 18 F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent
Author(s) -
Zhang Bo,
Fraser Benjamin H.,
Klenner Mitchell A.,
Chen Zhen,
Liang Steven H.,
Massi Massimiliano,
Robinson Andrea J.,
Pascali Giancarlo
Publication year - 2019
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201900930
Subject(s) - reagent , fluoride , fluorine , radiochemistry , solvent , cartridge , chemistry , inert , labelling , combinatorial chemistry , materials science , inorganic chemistry , organic chemistry , biochemistry , metallurgy
Fluorine‐18 is the most utilized radioisotope in positron emission tomography (PET), but the wide application of fluorine‐18 radiopharmaceuticals is hindered by its challenging labelling conditions. As such, many potentially important radiotracers remain underutilized. Herein, we describe the use of [ 18 F]ethenesulfonyl fluoride (ESF) as a novel radiofluoride relay reagent that allows radiofluorination reactions to be performed in minimally equipped satellite nuclear medicine centres. [ 18 F]ESF has a simple and reliable production route and can be stored on inert cartridges. The cartridges can then be shipped remotely and the trapped [ 18 F]ESF can be liberated by simple solvent elution. We have tested 18 radiolabelling precursors, inclusive of model and clinically used structures, and most precursors have demonstrated comparable radiofluorination efficiencies to those obtained using a conventionally dried [ 18 F]fluoride source.