Universität zu Köln

Hoffmann, Chris, Kolks, Niklas ORCID: 0000-0001-8532-0684, Smets, Daniel, Haseloer, Alexander ORCID: 0000-0003-0480-7568, Groener, Benedikt, Urusova, Elizaveta A., Endepols, Heike, Neumaier, Felix, Ruschewitz, Uwe ORCID: 0000-0002-6511-6894, Klein, Axel ORCID: 0000-0003-0093-9619, Neumaier, Bernd and Zlatopolskiy, Boris D. (2023). Next Generation Copper Mediators for the Efficient Production of F-18-Labeled Aromatics. Chem.-Eur. J., 29 (2). WEINHEIM: WILEY-V C H VERLAG GMBH. ISSN 1521-3765

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Abstract

Cu-mediated radiofluorination is a versatile tool for the preparation of F-18-labeled (hetero)aromatics. In this work, we systematically evaluated a series of complexes and identified several generally applicable mediators for highly efficient radiofluorination of aryl boronic and stannyl substrates. Utilization of these mediators in nBuOH/DMI or DMI significantly improved F-18-labeling yields despite use of lower precursor amounts. Impressively, application of 2.5 mu mol aryl boronic acids was sufficient to achieve F-18-labeling yields of up to 75 %. The practicality of the novel mediators was demonstrated by efficient production of five PET-tracers and transfer of the method to an automated radiosynthesis module. In addition, (S)-3-[F-18]FPhe and 6-[F-18]FDOPA were prepared in activity yields of 23 +/- 1 % and 30 +/- 3 % using only 2.5 mu mol of the corresponding boronic acid or trimethylstannyl precursor.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Hoffmann, Chris UNSPECIFIED UNSPECIFIED UNSPECIFIED Kolks, Niklas UNSPECIFIED orcid.org/0000-0001-8532-0684 UNSPECIFIED Smets, Daniel UNSPECIFIED UNSPECIFIED UNSPECIFIED Haseloer, Alexander UNSPECIFIED orcid.org/0000-0003-0480-7568 UNSPECIFIED Groener, Benedikt UNSPECIFIED UNSPECIFIED UNSPECIFIED Urusova, Elizaveta A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Endepols, Heike UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Felix UNSPECIFIED UNSPECIFIED UNSPECIFIED Ruschewitz, Uwe UNSPECIFIED orcid.org/0000-0002-6511-6894 UNSPECIFIED Klein, Axel UNSPECIFIED orcid.org/0000-0003-0093-9619 UNSPECIFIED Neumaier, Bernd UNSPECIFIED UNSPECIFIED UNSPECIFIED Zlatopolskiy, Boris D. UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-668611
DOI:	10.1002/chem.202202965
Journal or Publication Title:	Chem.-Eur. J.
Volume:	29
Number:	2
Date:	2023
Publisher:	WILEY-V C H VERLAG GMBH
Place of Publication:	WEINHEIM
ISSN:	1521-3765
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language 5-HT2A RECEPTOR ANTAGONIST; RADIOFLUORINATION; PET; F-18-FLUORINATION; FLUORINATION; ESTERS; ACIDS; F-18 Multiple languages Chemistry, Multidisciplinary Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/66861