A1 Refereed original research article in a scientific journal
Radiosynthesis of the norepinephrine transporter tracer [F-18]NS12137 via copper-mediated F-18-labelling
Authors: Salla Lahdenpohja, Thomas Keller, Johan Rajander, Anna K. Kirjavainen
Publisher: WILEY
Publication year: 2019
Journal: Journal of Labelled Compounds and Radiopharmaceuticals
Journal name in source: JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Journal acronym: J LABELLED COMPD RAD
Volume: 62
Issue: 6
First page : 259
Last page: 264
Number of pages: 6
ISSN: 0362-4803
eISSN: 1099-1344
DOI: https://doi.org/10.1002/jlcr.3717
Self-archived copy’s web address: https://research.utu.fi/converis/portal/detail/Publication/41204500
[F-18]NS12137 (exo-3-[(6-[F-18]fluoro-2-pyridyl)oxy]8-azabicyclo[3.2.1]octane) is a highly selective norepinephrine transporter (NET) tracer. NETs are responsible for the reuptake of norepinephrine and dopamine and are linked to several neurodegenerative and neuropsychiatric disorders. The aim of this study was to develop a copper-mediated F-18-fluorination method for the production of [F-18]NS12137 with straightforward synthesis conditions and high radiochemical yield and molar activity. [F-18]NS12137 was produced in two steps. Radiofluorination of [F-18]NS12137 was performed via a copper-mediated pathway starting with a stannane precursor and using [F-18]F- as the source of the fluorine-18 isotope. Deprotection was performed via acid hydrolysis. The radiofluorination reaction was nearly quantitative as was the deprotection based on HPLC analysis. The radiochemical yield of the synthesis was 15.1 +/- 0.5%. Molar activity of [F-18]NS12137 was up to 300 GBq/mu mol. The synthesis procedure is straightforward and can easily be automated and adapted for clinical production.
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