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| Hauptseite > Publikationsdatenbank > Efficient synthesis of [$^{18}$ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols > print |
| Hauptseite > Publikationsdatenbank > Efficient synthesis of [$^{18}$ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols > print |
| 001 | 824538 | ||
| 005 | 20210129225049.0 | ||
| 024 | 7 | _ | |a 10.1002/jlcr.3469 |2 doi |
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| 100 | 1 | _ | |a Cavani, Melanie |0 P:(DE-Juel1)144953 |b 0 |
| 245 | _ | _ | |a Efficient synthesis of [$^{18}$ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols |
| 260 | _ | _ | |a New York, NY [u.a.] |c 2017 |b Wiley |
| 336 | 7 | _ | |a article |2 DRIVER |
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| 520 | _ | _ | |a An improved high yielding radiosynthesis of the known thiol-reactive maleimide-containing prosthetic group1-[3-(2-[18F]fluoropyridine-3-yloxy)propyl]pyrrole-2,5-dione ([18F]FPyME) is described. The target compound was obtained by a two-step one-pot procedure starting from a maleimide-containing nitro-precursor that was protected as a Diels-Alder adduct with 2,5-dimethylfurane. Nucleophilic radiofluorination followed by heat induced deprotection through a Retro Diels Alder reaction yielded, after chromatographic isolation, [18F]FPyME with a radiochemical yield of 20% in about 60 min overall synthesis time. A variety of other [18F]fluoropyridine based maleimide-containing prosthetic groups should be accessible via the described synthetic strategy. |
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