Universität zu Köln

Orlovskaya, Victoriya V., Modemann, Daniel J., Kuznetsova, Olga F., Fedorova, Olga S. ORCID: 0000-0002-9122-9622, Urusova, Elizaveta A., Kolks, Niklas ORCID: 0000-0001-8532-0684, Neumaier, Bernd ORCID: 0000-0001-5425-3116, Krasikova, Raisa N. and Zlatopolskiy, Boris D. (2019). Alcohol-Supported Cu-Mediated F-18-Fluorination of Iodonium Salts under Minimalist Conditions. Molecules, 24 (17). BASEL: MDPI. ISSN 1420-3049

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Abstract

In the era of personalized precision medicine, positron emission tomography (PET) and related hybrid methods like PET/CT and PET/MRI gain recognition as indispensable tools of clinical diagnostics. A broader implementation of these imaging modalities in clinical routine is closely dependent on the increased availability of established and emerging PET-tracers, which in turn could be accessible by the development of simple, reliable, and efficient radiolabeling procedures. A further requirement is a cGMP production of imaging probes in automated synthesis modules. Herein, a novel protocol for the efficient preparation of F-18-labeled aromatics via Cu-mediated radiofluorination of (aryl)(mesityl) iodonium salts without the need of evaporation steps is described. Labeled aromatics were prepared in high radiochemical yields simply by heating of iodonium [F-18]fluorides with the Cu-mediator in methanolic DMF. The iodonium [F-18]fluorides were prepared by direct elution of F-18(-) from an anion exchange resin with solutions of the corresponding precursors in MeOH/DMF. The practicality of the novel method was confirmed by the racemization-free production of radiolabeled fluorophenylalanines, including hitherto unknown 3-[F-18]FPhe, in 22-69% isolated radiochemical yields as well as its direct implementation into a remote-controlled synthesis unit.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Orlovskaya, Victoriya V. UNSPECIFIED UNSPECIFIED UNSPECIFIED Modemann, Daniel J. UNSPECIFIED UNSPECIFIED UNSPECIFIED Kuznetsova, Olga F. UNSPECIFIED UNSPECIFIED UNSPECIFIED Fedorova, Olga S. UNSPECIFIED orcid.org/0000-0002-9122-9622 UNSPECIFIED Urusova, Elizaveta A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Kolks, Niklas UNSPECIFIED orcid.org/0000-0001-8532-0684 UNSPECIFIED Neumaier, Bernd UNSPECIFIED orcid.org/0000-0001-5425-3116 UNSPECIFIED Krasikova, Raisa N. UNSPECIFIED UNSPECIFIED UNSPECIFIED Zlatopolskiy, Boris D. UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-142310
DOI:	10.3390/molecules24173197
Journal or Publication Title:	Molecules
Volume:	24
Number:	17
Date:	2019
Publisher:	MDPI
Place of Publication:	BASEL
ISSN:	1420-3049
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language ONE-POT SYNTHESIS; DIARYLIODONIUM SALTS; CATALYZED FLUORINATION; PET; RADIOFLUORINATION; DERIVATIVES; REAGENT; IODINE Multiple languages Biochemistry & Molecular Biology; Chemistry, Multidisciplinary Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/14231