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KMID : 1145520170030020091
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Journal of Radiopharmaceuticals and Molecular Probes
2017 Volume.3 No. 2 p.91 ~ p.97
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An optimized radiosynthesis of 18F-THK-5351 for routine production on TRACERlab™ FXFN
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Park Jun-Young
Son Jeong-Min
Yun Mi-Jin
Chun Joong-Hyun
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Abstract
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18F-THK-5351 is a PET radiotracer to image the hyperphosphorylated tau fibrillar aggregates in human brain. This protocol describes the optimized radiosynthesis of 18F-THK-5351 using a commercial GE TRACERlab™ FXFN radiosynthesis module. 18F-THK-5351 was prepared by nucleophilic [18F]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 °C for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of 18F-THK-5351 was 31.9 ± 6.7%(decay-corrected, n = 10), with molar activity of 198.1 ± 33.9 GBq/μmol(5.4 ± 0.9 Ci/μmol, 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.
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KEYWORD
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18F-THK-5351, Tau imaging, Fluorine-18, PET, Radiotracer, Automation
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