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- Title
Practical microscale one‐pot radiosynthesis of <sup>18</sup>F‐labeled probes.
- Authors
Iwata, Ren; Pascali, Claudio; Terasaki, Kazunori; Ishikawa, Yoichi; Furumoto, Shozo; Yanai, Kazuhiko
- 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.
- Subjects
RADIOPHARMACEUTICALS; MEDICAL radiology; POSITRON emission tomography; POPULATION transfers; LEWIS acids
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2018, Vol 61, Issue 7, p540
- ISSN
0362-4803
- Publication type
Article
- DOI
10.1002/jlcr.3618