A novel [18F]fluoride relay reagent for radiofluorination reactions

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dc.contributor.authorZhang, Ben_AU
dc.contributor.authorFraser, BHen_AU
dc.contributor.authorKlenner, MAen_AU
dc.contributor.authorChen, Zen_AU
dc.contributor.authorLiang, SHen_AU
dc.contributor.authorMassi, Men_AU
dc.contributor.authorRobinson, AJen_AU
dc.contributor.authorPascali, Gen_AU
dc.date.accessioned2021-09-02T23:42:35Zen_AU
dc.date.available2021-09-02T23:42:35Zen_AU
dc.date.issued2019-05-26en_AU
dc.date.statistics2021-09-02en_AU
dc.descriptionVolume 62, Supplement 1 of the Journal of Labelled Compounds & Pharmaceuticals is comprised of the Abstracts from ISRS 2019.en_AU
dc.description.abstractObjectives 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. This necessitates production at centralized PET centres with highly specialized equipment including cyclotrons, hot cells, synthesizers, and HPLC capabilities, which ultimately limit the availability of fluorine‐18 tracers to those whose production has a large marketing scale (e.g., [18F]FDG). As such, many potentially important leads 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 (Figure 1). Methods [18F]ESF was produced from 2,4,6‐trichlorophenylethenesulfonate using a microfluidic system and was stored on inert cartridges. The cartridges could be shipped remotely where trapped [18F]ESF was liberated by chosen solvent to a vial containing precursor and additives. The reaction mixture was then stirred and heated using a heating block. Reaction conditions including temperature, time, precursor concentration, and additives were optimised, and the radiochemical yields (RCYs) were compared with those for traditional [18F]fluoride method. Results We found that conditions of 1 mg/mL precursor, 0.5 mg/mL tetraethylammonium bicarbonate as additive, temperature of 100°C, and time of 15 min were useful to assess radiofluorination scope on commercially available precursors. The obtained RCYs were compared with those generated from traditional dried [18F]fluoride source and no statically significant difference was observed for most precursors. Some differences on RCYs, both positive and negative, were noted when novel type of precursors (i.e., boronic acids, iodonium ylides) were tested. Conclusions We have developed a method to perform radiofluorinations using a new radiofluoride relay reagent, [18F] ESF. Such method reduces the reaction equipment needed, in the simplest case to a simple heating block, single‐use vials and magnetic stir bar. Notably, this new process is not only compatible with typical commercial precursors, but also feasible to accommodate emerging precursors with novel leaving groups. © 2019 The Authorsen_AU
dc.description.sponsorshipFinancial supports from Monash University (MGS and MIPRS) and The Australian Institute of Nuclear Science and Engineering (AINSE PGRA 12074) are gratefully acknowledged.en_AU
dc.identifier.citationZhang, B., Fraser, B., Klenner, M., Chen, Z., Liang, S., Massi, M., Robinson, A. & Pascali, G. (2019). A novel [18F]fluoride relay reagent for radiofluorination reactions. Poster presented at the 23rd International Symposium on Radiopharmaceutical Sciences (ISRS 2019), Beijing, China, 26 to 31 May, 2019. In Journal of Labelled Compounds and Radiopharmaceuticals, 62(S1), S123-S588. doi:10.1002/jlcr.3725en_AU
dc.identifier.conferenceenddate31 May 2019en_AU
dc.identifier.conferencename23rd International Symposium on Radiopharmaceutical Sciences (ISRS 2019)en_AU
dc.identifier.conferenceplaceBeijing, Chinaen_AU
dc.identifier.conferencestartdate26 May 2019en_AU
dc.identifier.issn1099-1344en_AU
dc.identifier.issueS1en_AU
dc.identifier.journaltitleJournal of Labelled Compounds and Radiopharmaceuticalsen_AU
dc.identifier.paginationS123-S588en_AU
dc.identifier.urihttps://doi.org/10.1002/jlcr.3725en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/11579en_AU
dc.identifier.volume62en_AU
dc.language.isoenen_AU
dc.publisherJohn Wiley & Sons, Incen_AU
dc.subjectFluoridesen_AU
dc.subjectRadioisotopesen_AU
dc.subjectPositron computed tomographyen_AU
dc.subjectRadiopharmaceuticalsen_AU
dc.subjectLabellingen_AU
dc.subjectLabelled compoundsen_AU
dc.titleA novel [18F]fluoride relay reagent for radiofluorination reactionsen_AU
dc.typeConference Posteren_AU
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