Literature DB >> 30977166

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

Bo Zhang1,2, Benjamin H Fraser1, Mitchell A Klenner1,3, Zhen Chen4, Steven H Liang4, Massimiliano Massi3, Andrea J Robinson2, Giancarlo Pascali1,5.   

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 [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.
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  fluorine; medicinal chemistry; positron emission tomography; radiopharmaceuticals; sulfonyl fluoride

Year:  2019        PMID: 30977166     DOI: 10.1002/chem.201900930

Source DB:  PubMed          Journal:  Chemistry        ISSN: 0947-6539            Impact factor:   5.236


  2 in total

1.  Rhenium(i) complexation-dissociation strategy for synthesising fluorine-18 labelled pyridine bidentate radiotracers.

Authors:  Mitchell A Klenner; Bo Zhang; Gianluca Ciancaleoni; James K Howard; Helen E Maynard-Casely; Jack K Clegg; Massimiliano Massi; Benjamin H Fraser; Giancarlo Pascali
Journal:  RSC Adv       Date:  2020-02-28       Impact factor: 4.036

2.  Late-Stage Copper-Catalyzed Radiofluorination of an Arylboronic Ester Derivative of Atorvastatin.

Authors:  Gonçalo S Clemente; Tryfon Zarganes-Tzitzikas; Alexander Dömling; Philip H Elsinga
Journal:  Molecules       Date:  2019-11-20       Impact factor: 4.411

  2 in total

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