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Optimization of the radiosynthesis of [ 18 F]MEFWAY for imaging brain serotonin 1A receptors by using the GE TracerLab FX FN‐Pro module
Author(s) -
Choi Jae Yong,
Kim Chul Hoon,
Ryu Young Hoon,
Seo Young Beom,
Truong Phong,
Kim Eun Jung,
Choi Tae Hyun,
Kang JeeHae,
Lee Minkyung,
Kim Dong Goo,
Lee Jong Doo,
Jeon Tae Joo
Publication year - 2013
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.3067
Subject(s) - chemistry , radiosynthesis , acetonitrile , methylamine , yield (engineering) , nuclear chemistry , methanol , extraction (chemistry) , radiochemistry , chromatography , organic chemistry , nuclear medicine , positron emission tomography , medicine , materials science , metallurgy
The aim of this study was to develop a highly reliable radiofluorination method for the preparation of N ‐{2‐[4‐(2‐methoxyphenyl)piperazinyl]ethyl}‐ N ‐(2‐pyridyl)‐ N ‐(4‐ 18 F‐fluoromethylcyclohexane)carboxamide ([ 18 F]Mefway) by using a fully automated system. The optimal condition is composed of two parts. The extraction system of the trapped F‐18 in the anion exchange resin (i.e., quaternary methylamine cartridge) is a complex of Kryptofix 2.2.2. (K222, 4 mg/0.9 mL methanol) and K 2 CO 3 (1 mg/0.1 mL H 2 O). After removing the solvents, the trans ‐tosylated Mefway precursor (1 mg/0.5 mL acetonitrile) was reacted with dried K222‐K[ 18 F] at 100°C for 5 min. After purification and formulation, [ 18 F]Mefway was obtained with 38 ± 2.4% (decay corrected, n = 34) radiochemical yield, a total synthesis time of 52 ± 3.4 min, specific activity was 120.6 ± 8.7 GBq/µmol at the end of synthesis and a radiochemical purity of 99%. According to the quality control tests, formulated [ 18 F]Mefway is suitable to apply parenteral clinical application.