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

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 fr...

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Published in:대한방사성의약품학회지, 3(2) 2017, 3(2), , pp.91-97
Main Authors: 박준영, 손정민, 윤미진, 전중현
Format: Article
Language:Korean
Subjects:
방사선과학
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Summary: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 KCI Citation Count: 0
ISSN:2384-1583
2508-3848