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000824538 1001_ $$0P:(DE-Juel1)144953$$aCavani, Melanie$$b0
000824538 245__ $$aEfficient synthesis of [$^{18}$ F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols
000824538 260__ $$aNew York, NY [u.a.]$$bWiley$$c2017
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000824538 520__ $$aAn 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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000824538 7001_ $$0P:(DE-Juel1)131810$$aBier, Dirk$$b1$$eCorresponding author$$ufzj
000824538 7001_ $$0P:(DE-Juel1)131824$$aHolschbach, Marcus$$b2$$ufzj
000824538 7001_ $$0P:(DE-Juel1)131816$$aCoenen, Heinrich Hubert$$b3$$ufzj
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