Telescoping the synthesis of the [18F]CABS13 Alzheimer's disease radiopharmaceutical via flow microfluidic rhenium(I) complexations

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dc.contributor.authorKlenner, MAen_AU
dc.contributor.authorFraser, BHen_AU
dc.contributor.authorMoon, Ven_AU
dc.contributor.authorEvans, BJen_AU
dc.contributor.authorMassi, Men_AU
dc.contributor.authorPascali, Gen_AU
dc.date.accessioned2021-09-08T22:54:41Zen_AU
dc.date.available2021-09-08T22:54:41Zen_AU
dc.date.issued2020-09-24en_AU
dc.date.statistics2021-09-07en_AU
dc.description.abstractThe syntheses of rhenium(I) complexes were achieved under flow microfluidic conditions. The use of a single microreactor was applied towards complexation of the 6-chloro-2,2'-bipyridine diimine ligand, with ideal complexation conditions around 170 °C. Subsequent radiolabelling with [18F]fluoride was further achieved by flowing through a second heated microreactor, alongside a stream of dried radiofluorination media. Temperature modulation across both microreactors resulted in 23.6 % and 37.0 % radiochemical yield (RCY) of [18F]6-fluoro-2,2'-bipyridine and its associated [18F]tricarbonyl(2-fluoro-2,2'-bipyridine)rhenium(I) chloride complex, respectively. Translation of this set-up to the synthesis of the [18F]CABS13 Alzheimer's disease positron emission tomography (PET) imaging agent was achieved with the incorporation of a third microreactor to enable thermal control of the complexation, fluorination and decomplexation pathways. Optimal RCYs of 2.7 % and 1.9 % of [18F]CABS13 and its rhenium(I) complexation were achieved in-flow, respectively. However, discrepancies in the RCYs were found to arise from differences in the grade of anhydrous dimethyl sulfoxide (DMSO) employed in the continuous-flow reactions. Anhydrous DMSO from Sigma-Aldrich (≤ 99.9 %) in former experiments afforded higher yielders in comparison to replicate experiments employing anhydrous DMSO from Merck Millipore (≤ 99.7 %), thus demonstrating that control of the solvent grade is key to optimizing reaction RCYs. © 2020 Wiley-VCH GmbHen_AU
dc.identifier.citationKlenner, M. A., Fraser, B. H., Moon, V., Evans, B. J., Massi, M., & Pascali, G. (2020). Telescoping the synthesis of the [18F] CABS13 Alzheimer's disease radiopharmaceutical via flow microfluidic rhenium (I) complexations. European Journal of Inorganic Chemistry, 2020(37), 3554-3564. doi:10.1002/ejic.202000433en_AU
dc.identifier.issn1099-0682en_AU
dc.identifier.issue37en_AU
dc.identifier.journaltitleEuropean Journal of Inorganic Chemistryen_AU
dc.identifier.pagination3554-3564en_AU
dc.identifier.urihttps://doi.org/10.1002/ejic.202000433en_AU
dc.identifier.urihttps://apo.ansto.gov.au/dspace/handle/10238/11652en_AU
dc.identifier.volume2020en_AU
dc.language.isoenen_AU
dc.publisherJohn Wiley & Sons, Incen_AU
dc.subjectNervous system diseasesen_AU
dc.subjectFluorine 18en_AU
dc.subjectFluoridesen_AU
dc.subjectRheniumen_AU
dc.subjectSynthesisen_AU
dc.subjectRadiopharmaceuticalsen_AU
dc.titleTelescoping the synthesis of the [18F]CABS13 Alzheimer's disease radiopharmaceutical via flow microfluidic rhenium(I) complexationsen_AU
dc.typeJournal Articleen_AU
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