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A one‐step automated synthesis of the dopamine transporter ligand [ 18 F]FECNT from the chlorinated precursor
Author(s) -
PijarowskaKruszyna Justyna,
Jaron Antoni,
Kachniarz Artur,
Malkowski Bogdan,
Garnuszek Piotr,
Mikolajczak Renata
Publication year - 2016
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.3375
Subject(s) - chemistry , radiosynthesis , yield (engineering) , dopamine transporter , ligand (biochemistry) , radiochemistry , nucleophile , chemical synthesis , nucleophilic substitution , specific activity , biodistribution , nuclear chemistry , medicinal chemistry , transporter , organic chemistry , nuclear medicine , catalysis , in vitro , positron emission tomography , medicine , biochemistry , materials science , receptor , gene , metallurgy , enzyme
The use of [ 18 F]labelled nortropane derivative 2 β ‐carbomethoxy‐3 β ‐(4‐chlorophenyl)‐8‐(2‐fluoroethyl)‐nortropane (FECNT) as a dopamine transporter ligand for PET imaging is dependent on efficient radiosynthesis method. Herein, the automated synthesis of [ 18 F]FECNT from its chlorinated precursor in commercially available SynChrom [ 18 F] R&D module has been developed. The synthesis unit was readily configured for the one‐step synthesis from corresponding chlorinated precursor. The radiolabeling process involved a classical [ 18 F]fluoride nucleophilic substitution performed at 110 °C for 12 min and finally HPLC and SPE purification. Crude [ 18 F]FECNT was obtained with a radiolabeling yield of 59 ± 12% ( n = 5). The average uncorrected amount of [ 18 F]FECNT in the final formulated dose was 2.0 ± 0.5 GBq (32 ± 7% overall decay‐corrected yields) obtained with radiochemical purity over 99% and specific activity of 55 GBq/µmol. The total duration of the procedure was 80–90 min. An automated radiosynthesis of [ 18 F]FECNT with high radiochemical purity may provide a simple and robust method of radiopharmaceutical preparation for routine clinical applications.