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http://dx.doi.org/10.22643/kisti.2017.3.2.91

An optimized radiosynthesis of 18F-THK-5351 for routine production on TRACERlab™ FXFN  

Park, Jun Young (Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System)
Son, Jeongmin (Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System)
Yun, Mijin (Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System)
Chun, Joong-Hyun (Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System)
Publication Information
Journal of Radiopharmaceuticals and Molecular Probes / v.3, no.2, 2017 , pp. 91-97 More about this Journal
Abstract
$^{18}F-THK-5351$ is a PET radiotracer to image the hyperphosphorylated tau fibrillar aggregates in human brain. This protocol describes the optimized radiosynthesis of $^{18}F-THK-5351$ using a commercial GE $TRACERlab^{TM}$ $FX_{FN}$ radiosynthesis module. $^{18}F-THK-5351$ was prepared by nucleophilic [$^{18}F$]fluorination from its protected tosylate precursors, (S)-(2-(2-methylaminopyrid-5-yl)-6-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy] quinolone(THK-5352), at $110^{\circ}C$ for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of $^{18}F-THK-5351$ was $31.9{\pm}6.7%$(decay-corrected, n = 10), with molar activity of $198.1{\pm}33.9GBq/{\mu}mol$($5.4{\pm}0.9Ci/{\mu}mol$, n = 10). The radiochemical purity was determined to be above 98%. The overall production time including HPLC purification is approximately 70 min. This fully-automated protocol is validated for clinical use.
Keywords
$^{18}F-THK-5351$; Tau imaging; Fluorine-18; PET; Radiotracer; Automation;
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