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| Hauptseite > Publikationsdatenbank > Protocol for Automated Production of Radiofluorinated Boramino Acids |
| Hauptseite > Publikationsdatenbank > Protocol for Automated Production of Radiofluorinated Boramino Acids |
| Contribution to a conference proceedings/Journal Article | FZJ-2026-03766 |
; ; ;
2025
Elsevier Science
Amsterdam [u.a.]
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Please use a persistent id in citations: doi:10.1016/j.nucmedbio.2025.109207
Abstract: Introduction: Radiofluorinated boramino acids ([18F]BAAs) have emerged as promising alternatives to established amino acid PET tracers, since they offer high metabolic stability and high affinity to amino acid transporters (1). However, despite encouraging results of first-in-man studies, no procedures for automated production of [18F]BAAs have been reported to date.(2) Hence, this study aimed to develop an optimized protocol for automated production of the 18F-labeled leucine and proline analogs [18F]LeuBF3 and [18F]ProBF3. Methods: [18F]LeuBF3 and [18F]ProBF3 were synthesized via 18F/19F isotopic exchange and the labeling conditions were optimized with respect to precursor amount, pH, reaction time, temperature, solvent, acid/buffer, and pressure. The optimized conditions were then transferred to a Trasis AllInOne automated radiosynthesis module. Results: Under conditions optimized for manual radiosyntheses (100 nmol LeuBF3, 0.25 M TFA in 100 μL EtOH, 30 minutes at 100 °C), [18F]LeuBF3 was synthesized with radiochemical conversions (RCCs) of 47 ± 11% (n = 3). The small reaction volume of 100 μL was, however, not well compatible with conventional automated synthesis modules. Accordingly, reaction conditions were modified to apply 150 nmol LeuBF3, 0.09 M TFA in 700 μL EtOH, and reaction pressure of 750 bar until complete evaporation of EtOH. These conditions yielded [18F]LeuBF3 with activity yields (AYs) of 22 ± 1% in manual radiosyntheses. Upon transfer to the Trasis AllInOne, further optimization of reaction temperature and pressure (115 °C and 500 mbar, respectively) was required. This enabled automated production of [18F]LeuBF3 and [18F]ProBF3 with AYs of 10–15% (n = 2) and 18–20% (n = 2), respectively. Isolation by solid phase extraction (Alum N cartridges) or HPLC (Phenomenex Synergy Hydro-RP columns with mixtures of PBS/EtOH as mobile phase) afforded the [18F]BAAs with (radio)chemical purities of >98% within 25–30 minutes. Conclusions: A cGMP-compliant protocol for automated production of [18F]BAAs in amounts sufficient for (pre)clinical applications was established.
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