title: A one-step automated synthesis of the dopamine transporter ligand [(18)F]FECNT from the chlorinated precursor.
abstract: The use of [(18)F]labelled nortropane derivative 2β-carbomethoxy-3β-(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.
authors: National Centre for Nuclear Research, Radioisotope Centre POLATOM, Andrzeja Soltana 7, Otwock, 05-400, Poland.
authors: Justyna
authors: J
authors: Pijarowska-Kruszyna
authors: National Centre for Nuclear Research, Radioisotope Centre POLATOM, Andrzeja Soltana 7, Otwock, 05-400, Poland.
authors: Antoni
authors: A
authors: Jaron
authors: Department of Nuclear Medicine, Oncology Centre Prof. Lukaszczyk Memorial Hospital, Bydgoszcz, Poland.
authors: Artur
authors: A
authors: Kachniarz
authors: Department of Nuclear Medicine, Oncology Centre Prof. Lukaszczyk Memorial Hospital, Bydgoszcz, Poland.
authors: Bogdan
authors: B
authors: Malkowski
authors: National Centre for Nuclear Research, Radioisotope Centre POLATOM, Andrzeja Soltana 7, Otwock, 05-400, Poland.
authors: Piotr
authors: P
authors: Garnuszek
authors: National Centre for Nuclear Research, Radioisotope Centre POLATOM, Andrzeja Soltana 7, Otwock, 05-400, Poland.
authors: Renata
authors: R
authors: Mikolajczak
mesh_terms: D009662:Nortropanes / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
chemical_list: C410211:2-carbomethoxy-3-(4-chlorophenyl)-8-(2-fluoroethyl)nortropane; D009662:Nortropanes; D019275:Radiopharmaceuticals
keywords: [18F]FECNT; automated synthesis; dopamine transporter (DAT); modular synthesis unit