Premium
Radiosynthesis of the norepinephrine transporter tracer [ 18 F]NS12137 via copper‐mediated 18 F ‐labelling
Author(s) -
Lahdenpohja Salla,
Keller Thomas,
Rajander Johan,
Kirjavainen Anna K.
Publication year - 2019
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3717
Subject(s) - chemistry , radiosynthesis , labelling , yield (engineering) , norepinephrine transporter , reuptake , norepinephrine , tracer , hydrolysis , copper , chemical synthesis , radiochemistry , octane , dopamine , transporter , organic chemistry , in vitro , in vivo , biochemistry , serotonin , materials science , receptor , microbiology and biotechnology , physics , neuroscience , gene , nuclear physics , metallurgy , biology
[ 18 F]NS12137 ( exo ‐3‐[(6‐[ 18 F]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 18 F‐fluorination method for the production of [ 18 F]NS12137 with straightforward synthesis conditions and high radiochemical yield and molar activity. [ 18 F]NS12137 was produced in two steps. Radiofluorination of [ 18 F]NS12137 was performed via a copper‐mediated pathway starting with a stannane precursor and using [ 18 F]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 [ 18 F]NS12137 was up to 300 GBq/μmol. The synthesis procedure is straightforward and can easily be automated and adapted for clinical production.