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KMID : 1148920220560020086
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Nuclear Medicine and Molecular Imaging
2022 Volume.56 No. 2 p.86 ~ p.95
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Improved Stability and Practicality for Synthesis of 4-Borono-2-[18F]fluoro-L-phenylalanine by Combination of [18O]O2 Single-Use and [18F]CH3COOF Labeling Agents
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Naka Sadahiro
Watanabe Toshimitsu
Kanai Yasukazu
Watabe Tadashi
Tatsumi Mitsuaki
Kato Hiroki
Shimosegawa Eku
Hatazawa Jun
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Abstract
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Purpose: 4-Borono-2-[18F]fluoro-L-phenylalanine ([18F]FBPA) synthesized with [18F]F2, produced using the 18O(p, n)18F reaction, has been reported for increasing radioactivity. However, a dedicated system and complex procedure is required to reuse the costly [18O]O2 gas; also, the use of [18F]F2 as a labeling agent reduces the labeling rate and radiochemical purity. We developed a stable and practical method for [18F]FBPA synthesis by combining [18F]F2, produced using a [18O]O2 single-use system, and a [18F]CH3COOF labeling agent.
Methods: The produced [18F]F2 was optimized, and then [18F]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 [18O]O2 gas, and then irradiated (first irradiation). Then, the [18O]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 CH3COONa column, converting it into the [18F]CH3COOF labeling agent, which was then used for [18F]FBPA synthesis.
Results: The mean amount of as-obtained [18F]F2 was 55.0 ± 3.3 GBq and that of as-obtained [18F]CH3COOF was 21.6 ± 1.4 GBq after the bombardment. The radioactivity and the radiochemical yield based on [18F]F2 of [18F]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 [18F]FBPA production, which is more stable and practical compared with the method using [18O]O2 gas-recycling and [18F]F2 labeling agent.
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KEYWORD
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[18O]O2 gas, Single-use, [18F]F2, [18F]CH3COOF, [18F]FBPA, Boron neutron capture therapy
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