Rapid 18 F-labeling via Pd-catalyzed S-arylation in aqueous medium

Rapid 18 F-labeling via Pd-catalyzed S-arylation in aqueous medium

We report radiolabeling of thiol-containing substrates via Pd-catalyzed S-arylation with 2-[ F]fluoro-5-iodopyridine, which is readily accessible using the "minimalist" radiofluorination method. The practicality of the procedure was confirmed by preparation of a novel PSMA-specific PET-tra...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2021-04, Vol.57 (29), p.3547-3550
Hauptverfasser: Humpert, Swen, Omrane, Mohamed A, Urusova, Elizaveta A, Gremer, Lothar, Willbold, Dieter, Endepols, Heike, Krasikova, Raisa N, Neumaier, Bernd, Zlatopolskiy, Boris D
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Sprache:eng
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Zusammenfassung:We report radiolabeling of thiol-containing substrates via Pd-catalyzed S-arylation with 2-[ F]fluoro-5-iodopyridine, which is readily accessible using the "minimalist" radiofluorination method. The practicality of the procedure was confirmed by preparation of a novel PSMA-specific PET-tracer as well as labeling of glutathione, Aβ oligomer-binding RD2 peptide, bovine serum albumin and PSMA I&S.
ISSN:1359-7345
1364-548X
DOI:10.1039/D1CC00745A