Nucl Med Mol Imaging.
2022 Apr;56(2):86-95. 10.1007/s13139-021-00719-1.
Improved Stability and Practicality for Synthesis of 4-Borono-2-[ 18F] fluoro-L-phenylalanine by Combination of [ 18 O]O 2 Single-Use and [ 18 F]CH 3 COOF Labeling Agents
- Affiliations
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- 1Department of Nuclear Medicine and Tracer Kinetics, Graduate School of Medicine, Osaka University, 2-2, Yamadaoka, Suita, Osaka 565-0871, Japan
- 2Department of Radiology, Osaka University Hospital, 2-15, Yamadaoka, Suita, Osaka 565-0871, Japan
- 3Radiochemistry and Targetry Section, Engineering Department, Medical & Advanced Equipment Unit, Industrial Equipment Division, Sumitomo Heavy Industries, 5-2, Soubiraki-cho, Niihama, Ehime 792-8588, Japan
- 4Department of Biofunctional Analysis, Faculty of Pharmacy, Osaka Medical and Pharmaceutical University, 4-20-1, Nasahara, Takatsuki, Osaka 569-1094, Japan
- 5Department of Quantum Cancer Therapy, Research Center for Nuclear Physics, Osaka University, 10-1, Mihogaoka, Osaka, Ibaraki 567-0047, Japan
- 6Department of Molecular Imaging in Medicine, Graduate School of Medicine, Osaka University, 2-2, Yamadaoka, Suita, Osaka 565-0871, Japan
- KMID: 2528459
- DOI: http://doi.org/10.1007/s13139-021-00719-1
Abstract
- Purpose
4-Borono-2-[ 18 F]fluoro-L-phenylalanine ([ 18 F]FBPA) synthesized with [ 18 F]F2 , produced using the 18 O(p, n) 18 F reaction, has been reported for increasing radioactivity. However, a dedicated system and complex procedure is required to reuse the costly [ 18 O]O2 gas; also, the use of [ 18 F]F2 as a labeling agent reduces the labeling rate and radiochemical purity. We developed a stable and practical method for [ 18 F]FBPA synthesis by combining [ 18 F]F2 , produced using a [ 18 O]O2 single-use system, and a [ 18 F]CH3 COOF labeling agent.
Methods
The produced [ 18 F]F2 was optimized, and then [ 18 F]FBPA was synthesized. For passivation of the target box, 0.5% F2 was pre-irradiated in argon. Gaseous products were discarded; the target box was filled with [ 18 O]O2 gas, and then irradiated (first irradiation). Then, the [ 18 O]O2 gas was discarded, 0.05–0.08% F2 in argon was fed into the target box, and it was again irradiated (second irradiation). The [ 18F]F2 obtained after this was passed through a CH3 COONa column, converting it into the [ 18 F]CH 3 COOF labeling agent, which was then used for [ 18 F]FBPA synthesis.
Results
The mean amount of as-obtained [ 18F]F2 was 55.0 ± 3.3 GBq and that of as-obtained [ 18 F]CH 3 COOF was 21.6 ± 1.4 GBq after the bombardment. The radioactivity and the radiochemical yield based on [ 18 F]F2 of [ 18 F]FBPA were 4.72 ± 0.34 GBq and 12.2 ± 0.1%, respectively. The radiochemical purity and molar activity were 99.3 ± 0.1% and 231 ± 22 GBq/mmol, respectively.
Conclusion
We developed a method for [ 18 F]FBPA production, which is more stable and practical compared with the method using [ 18 O]O2 gas-recycling and [ 18 F]F2 labeling agent.
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