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

 Jun Young Park  ;  Jeongmin Son  ;  Mijin Yun  ;  Joong-Hyun Chun 
 Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지), Vol.3(2) : 91-97, 2017 
Journal Title
 Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지) 
Issue Date
18F−THK−5351 ; Tau imaging ; Fluorine-18 ; PET ; Radiotracer ; Automation
18F−THK−5351 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 18F−THK−5351 using a commercial GE TRACERlabTM TRACERlabTM FXFN FXFN radiosynthesis module. 18F−THK−5351 18F−THK−5351 was prepared by nucleophilic [18F 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 110∘C for 10 min in dimethyl sulfoxide, followed by deprotection with 1 N HCl. The average radiochemical yield of 18F−THK−5351 18F−THK−5351 was 31.9±6.7 31.9±6.7 (decay-corrected, n = 10), with molar activity of 198.1±33.9GBq/μmol 198.1±33.9GBq/μmol (5.4±0.9Ci/μmol 5.4±0.9Ci/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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7. Others (기타) > Others (기타) > 1. Journal Papers
1. College of Medicine (의과대학) > Dept. of Nuclear Medicine (핵의학교실) > 1. Journal Papers
Yonsei Authors
Park, Jun Young(박준영) ORCID logo https://orcid.org/0000-0003-3403-2767
Yun, Mi Jin(윤미진) ORCID logo https://orcid.org/0000-0002-1712-163X
Chun, Joong-Hyun(전중현) ORCID logo https://orcid.org/0000-0002-9665-7829
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