Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Aliphatic radiofluorination using TBAHCO3 eluate in hydrous organic medium

  • Kwon, Young-Do (Department of Nuclear Medicine, Yonsei University College of Medicine) ;
  • Son, Jeongmin (Department of Nuclear Medicine, Severance Hospital, Yonsei University Health System) ;
  • Chun, Joong-Hyun (Department of Nuclear Medicine, Yonsei University College of Medicine)
  • Received : 2018.12.06
  • Accepted : 2018.12.21
  • Published : 2018.12.30
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Abstract

Azeotropic drying process is routinely applied to enhance nucleophilicity of $[^{18}F]$fluoride ion during the nucleophilic production of PET radiotracers; however, the drying process requires usually 15-25 min. Due to the high demand of employing fluorine-18 ($t_{1/2}=109.8min$) in PET radiopharmaceutical production, several research groups have focused on the method development, obviating tedious removal process of the residual target water ($[^{18}O]H_2O$) for $[^{18}F]$fluoride ion complex to be used in radiofluorination. Some development in radiofluorination in a mixed organic solvent system was demonstrated with various aliphatic substrates, but only kryptand as a phase transfer agent was utilized in the reported method. Here, we extend to investigate the development scope of applicability with basic alkyl ammonium salt as a phase transfer agent through the extensive elution efficiency study and radiofluorination outcome for aliphatic radiofluorination.

Keywords

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Figure 2. Representative radio-HPLC (coinjected with the authentic compound) and radio-TLC chromatogram.

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Figure 1. Elution efficiency with different PTA amount in Table 2.

Table 1. Comparison of elution efficiency with different phase transfer agents and organic solventsa)

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Table 2. Study of elution efficiency with different amount of PTA eluentaa)

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Table 3. Effect of total organic content on elution efficiency

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Table 4. Radiofluorination with different organic content in reaction medium (DMSO)a)

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