A one-step automated synthesis of the dopamine transporter ligand [18F]FECNT from the chlorinated precursor.

Autor: Pijarowska ‐ Kruszyna, Justyna, Jaron, Antoni, Kachniarz, Artur, Malkowski, Bogdan, Garnuszek, Piotr, Mikolajczak, Renata
Předmět:
Zdroj: Journal of Labelled Compounds & Radiopharmaceuticals; Mar2016, Vol. 59 Issue 3, p82-86, 5p
Abstrakt: The use of [18F]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 [18F]FECNT from its chlorinated precursor in commercially available SynChrom [18F] 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 [18F]fluoride nucleophilic substitution performed at 110 °C for 12 min and finally HPLC and SPE purification. Crude [18F]FECNT was obtained with a radiolabeling yield of 59 ± 12% ( n = 5). The average uncorrected amount of [18F]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 [18F]FECNT with high radiochemical purity may provide a simple and robust method of radiopharmaceutical preparation for routine clinical applications. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index