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| 100 | 1 | _ | |a Zarrad, Fadi |0 P:(DE-Juel1)166309 |b 0 |u fzj |
| 245 | _ | _ | |a A Practical Method for the Preparation of 18F-Labeled Aromatic Amino Acids from Nucleophilic [18F]Fluoride and Stannyl Precursors for Electrophilic Radiohalogenation |
| 260 | _ | _ | |a Basel |c 2017 |b MDPI75390 |
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| 520 | _ | _ | |a In a recent contribution of Scott et al., the substrate scope of Cu-mediated nucleophilic radiofluorination with [18F]KF for the preparation of 18F-labeled arenes was extended to aryl- and vinylstannanes. Based on these findings, the potential of this reaction for the production of clinically relevant positron emission tomography (PET) tracers was investigated. To this end, Cu-mediated radiofluorodestannylation using trimethyl(phenyl)tin as a model substrate was re-evaluated with respect to different reaction parameters. The resulting labeling protocol was applied for 18F-fluorination of different electron-rich, -neutral and -poor arylstannyl substrates in RCCs of 16–88%. Furthermore, this method was utilized for the synthesis of 18F-labeled aromatic amino acids from additionally N-Boc protected commercially available stannyl precursors routinely applied for electrophilic radiohalogenation. Finally, an automated synthesis of 6-[18F]fluoro-l-m-tyrosine (6-[18F]FMT), 2-[18F]fluoro-l-tyrosine (2-[18F]F-Tyr), 6-[18F]fluoro-l-3,4-dihydroxyphenylalanine (6-[18F]FDOPA) and 3-O-methyl-6-[18F]FDOPA ([18F]OMFD) was established furnishing these PET probes in isolated radiochemical yields (RCYs) of 32–54% on a preparative scale. Remarkably, the automated radiosynthesis of 6-[18F]FDOPA afforded an exceptionally high RCY of 54 ± 5% (n = 5). |
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| 700 | 1 | _ | |a Zlatopolskiy, Boris |0 P:(DE-HGF)0 |b 1 |
| 700 | 1 | _ | |a Krapf, Philipp |0 P:(DE-Juel1)169356 |b 2 |u fzj |
| 700 | 1 | _ | |a Zischler, Johannes |0 P:(DE-Juel1)166483 |b 3 |
| 700 | 1 | _ | |a Neumaier, Bernd |0 P:(DE-Juel1)166419 |b 4 |e Corresponding author |u fzj |
| 773 | _ | _ | |a 10.3390/molecules22122231 |g Vol. 22, no. 12, p. 2231 - |0 PERI:(DE-600)2008644-1 |n 12 |p 2231 - |t Molecules |v 22 |y 2017 |x 1420-3049 |
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