Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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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)
  • Received : 2017.12.08
  • Accepted : 2017.12.28
  • Published : 2017.12.30
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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.

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References

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