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

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

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)7613-7617
Number of pages5
JournalChemistry - A European Journal
Volume25
Issue number32
DOIs
Publication statusPublished - 7 Jun 2019

Keywords

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

Cite this

Zhang, B., Fraser, B. H., Klenner, M. A., Chen, Z., Liang, S. H., Massi, M., Robinson, A. J., & Pascali, G. (2019). [18F]Ethenesulfonyl Fluoride as a Practical Radiofluoride Relay Reagent. Chemistry - A European Journal, 25(32), 7613-7617. https://doi.org/10.1002/chem.201900930