[18 F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent

Authors

Bo Zhang, Benjamin H. Fraser, Mitchell A. Klenner, Zhen Chen, Steven H. Liang, Massimiliano Massi, Andrea J. Robinson, Giancarlo Pascali

Published Chemistry – A European Journal
Graphical abstract
Abstract

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 [18F]ethenesulfonyl fluoride (ESF) as a novel radiofluoride relay reagent that allows radiofluorination reactions to be performed in minimally equipped satellite nuclear medicine centres. [18F]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 [18F]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 [18F]fluoride source.

Citation

B. Zhang, B. H. Fraser, M. A. Klenner, Z. Chen, S. H. Liang, M Massi, A. J. Robinson, G. Pascali, “[ 18 F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent”, Chemistry – A European Journal, 2019, 25(32), 7613-7617

Pdf  
Doi

https://doi.org/10.1002/chem.201900930

Keywords

fluorine, medicinal chemistry, positron emission tomography, radiopharmaceuticals, sulfonyl fluoride

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