Practical microscale one-pot radiosynthesis of 18F-labeled probes

Ren Iwata, Claudio Pascali, Kazunori Terasaki, Yoichi Ishikawa, Shozo Furumoto, Kazuhiko Yanai

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)

Abstract

High specific activity is often a significant requirement for radiopharmaceuticals. To achieve that with fluorine-18 (18F)-labeled probes, it is mandatory to start from no-carrier–added fluoride and to reduce to a minimum the amount of precursor in order to decrease the presence of any pseudocarrier. In the present study, a feasible and efficient method for microscale one-pot radiosynthesis of 18F-labeled probes is described. It allows a substantial reduction in precursor, solvent, and reagents, thus reducing also possible side reaction in the case of base-sensitive precursors. The method is based on the use of a small amount of Kryptofix 2.2.2/potassium [18F]fluoride in MeOH (K.222/K[18F]F-MeOH) obtained using Oasis MAX and MCX cartridges. Five methods, differing in terms of MeOH evaporation and precursor addition, for the radiosynthesis of [18F]fallypride and [18F]FET in ≤50-μL scale, were examined and evaluated. The method using the addition of DMSO to the K.222/K[18F]F-MeOH solution prior to MeOH evaporation is proposed as a versatile procedure for feasible one-pot 10- to 20-μL scale radiosyntheses. This method was successfully applied also to the radiosynthesis of [18F]FES, [18F]FLT, and [18F]FMISO, with radiochemical yields comparable with those reported in the literature. Purification of a crude product by an analytical HPLC column was also demonstrated.

Original languageEnglish
Pages (from-to)540-549
Number of pages10
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume61
Issue number7
DOIs
Publication statusPublished - 2018 Jun 15

Keywords

  • [F]FET
  • [F]fallypride
  • microscale radiosynthesis
  • reactive [F]fluoride

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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