@misc{oai:repo.qst.go.jp:00071724,
 author = {Kawamura, Kazunori and Kumata, Katsushi and Furutsuka, Kenji and Shiomi, Satoshi and Fujishiro, Tomoya and Ryuji, Watanabe and Takei, Makoto and Hashimoto, Hiroki and Ito, Takehito and Ogawa, Masanao and Igarashi, Nobuyuki and Muto, Masatoshi and Nengaki, Nobuki and Nemoto, Kazuyoshi and Zhang, Ming-Rong and 河村 和紀 and 熊田 勝志 and 古塚 賢士 and 潮見 聡 and 藤代 智也 and 渡辺 竜二 and 武井 誠 and 橋本 裕輝 and 伊藤 岳人 and 小川 政直 and 五十嵐 延行 and 武藤 正敏 and 念垣 信樹 and 根本 和義 and 張 明栄},
 month = {May},
 note = {Objectives: Translocator protein (18 kDa) (TSPO), a nucleus-encoded mitochondrial target transmembrane protein,
has been indicated as an active participant in the modulation of mitochondrial function. PET using radiolabeled TSPO
probes has allowed non-invasive and reliable investigation of TSPO in neuropathological damages of experimental
animals and humans. Many PET probes for TSPO imaging have been developed. Among them, [18F]FEDAC has
potent binding affinity and selectivity for TSPO [1], high signal to neuroinflammation [2], and high sensitivity and
specificity for detection of fatty liver diseases progression [3]. We had previously synthesized [18F]FEDAC by reaction
of desmethyl-precursor with [18F]fluoroethyl bromide at two steps using a modified 18F-labelling synthesizer
developed in our institute [1-3]. In this study, we simplified the synthesis of [18F]FEDAC by direct 18F-fluorination
using a typical 18F-labelling synthesizer to transfer the preparation of [18F]FEDAC to other institutes toward
multicenter clinical study.
Methods: Tosylate-precursor for radiosynthesis of [18F]FEDAC was synthesized according to the procedures, as
shown in Fig. 1. [18F]FEDAC was prepared by heating the tosylate-precursor with 18F- in DMSO at 110 ⁰C for 10-15
min.
Results: Tosylate-precursor of [18F]FEDAC was successfully synthesized from desmethyl-precursor. [18F]FEDAC
was obtained with sufficient radioactivity and suitable quality for injection in clinical application. The synthesis of [18
F]FEDAC was reproduceble to achieve >740 MBq, >300 GBq/μmol and >97% of radiochemical purity within 70 min of
an overall synthesis time. All other analytical results were in compliance with our in-house quality control and
assurance specifications.
Conclusions: We successfully synthesized [18F]FEDAC by fluorination of the tosylate-precursor with 18F- using onepot
18F-labelling synthesizer. This radioligand will be used in clinical study.
References: [1] Yanamoto K, et al (2009), Bioorg Med Chem Lett, 19, 1707-10. [2] Yui J, et al (2010), J Nucl Med, 51,
1301-9. [3] Xie L, et al (2012), J Hepatol, 57, 1076-82., 21st International Symposium on Radiopharmaceutical Sciences},
 title = {One-pot radiosynthesis of [18F]FEDAC as a clinically applicable PET ligand for imaging TSPO.},
 year = {2015}
}