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

Swen Humpert; Mohamed A. Omrane; Elizaveta A. Urusova; Lothar Gremer; Dieter Willbold; Heike Endepols; Raisa N. Krasikova; Bernd Neumaier; Boris D. Zlatopolskiy

doi:10.1039/D1CC00745A

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

Swen Humpert,

‡^a Mohamed A. Omrane,‡^ab Elizaveta A. Urusova,^ab Lothar Gremer,

^cd Dieter Willbold,

^cd Heike Endepols,

^abe Raisa N. Krasikova,

^fg Bernd Neumaier

*^ab and Boris D. Zlatopolskiy

^ab

Author affiliations

* Corresponding authors

^a Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Forschungszentrum Jülich GmbH, Jülich 52428, Germany
E-mail: b.neumaier@fz-juelich.de

^b Institute of Radiochemistry and Experimental Molecular Imaging, University Hospital Cologne, Cologne 50931, Germany

^c Institute of Biological Information Processing, Structural Biochemistry (IBI-7), Forschungszentrum Jülich, Jülich 52425, Germany

^d Institut für Physikalische Biologie, Heinrich-Heine-Universität Düsseldorf, Düsseldorf 40225, Germany

^e Department of Nuclear Medicine, University Hospital Cologne, Cologne 50937, Germany

^f N. P. Bechtereva Institute of the Human Brain, St.-Petersburg 197376, Russia

^g St.-Petersburg State University, St.-Petersburg 199034, Russia

Abstract

We report radiolabeling of thiol-containing substrates via Pd-catalyzed S-arylation with 2-[¹⁸F]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.

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DOI: https://doi.org/10.1039/D1CC00745A
Article type: Communication
Submitted: 08 Feb 2021
Accepted: 15 Mar 2021
First published: 15 Mar 2021
This article is Open Access

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Chem. Commun., 2021,57, 3547-3550

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

S. Humpert, M. A. Omrane, E. A. Urusova, L. Gremer, D. Willbold, H. Endepols, R. N. Krasikova, B. Neumaier and B. D. Zlatopolskiy, Chem. Commun., 2021, 57, 3547 DOI: 10.1039/D1CC00745A

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Chemical Communications

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

Abstract

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

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