Synthesis of 18F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[18F]fluoroiodobenzene as radiotracers for positron emission tomography (PET)

Frank R. Wüst; Aileen Höhne; Peter Metz

doi:10.1039/B412871K

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Synthesis of ¹⁸F-labelled cyclooxygenase-2 (COX-2) inhibitorsvia Stille reaction with 4-[¹⁸F]fluoroiodobenzene as radiotracers for positron emission tomography (PET)

Frank R. Wüst,*^a Aileen Höhne^a and Peter Metz^b

Author affiliations

* Corresponding authors

^a Institute of Bioinorganic and Radiopharmaceutical Chemistry, FZ-Rossendorf, PF 51 01 19, Dresden, Germany
E-mail: f.wuest@fz-rossendorf.de
Fax: +493512602951
Tel: +493512602760

^b Institute of Organic Chemistry, Technical University Dresden, Bergstraße 66, Dresden, Germany
E-mail: peter.metz@chemie.tu-dresden.de
Fax: +4935146333162
Tel: +4935146337006

Abstract

The Stille reaction with 4-[¹⁸F]fluoroiodobenzene as a novel approach for the synthesis of radiotracers for monitoring COX-2 expression by means of PET has been developed. Optimized reaction conditions were elaborated by screening of various catalyst systems and solvents. By using optimized reaction conditions ¹⁸F-labelled COX-2 inhibitors [¹⁸F]-5 and [¹⁸F]-13 could be obtained in radiochemical yields of up to 94% and 68%, respectively, based upon 4-[¹⁸F]fluoroiodobenzene.

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Article information

DOI: https://doi.org/10.1039/B412871K
Article type: Paper
Submitted: 20 Aug 2004
Accepted: 15 Nov 2004
First published: 22 Dec 2004

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Org. Biomol. Chem., 2005,3, 503-507

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Synthesis of ¹⁸F-labelled cyclooxygenase-2 (COX-2) inhibitors via Stille reaction with 4-[¹⁸F]fluoroiodobenzene as radiotracers for positron emission tomography (PET)

F. R. Wüst, A. Höhne and P. Metz, Org. Biomol. Chem., 2005, 3, 503 DOI: 10.1039/B412871K

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Organic & Biomolecular Chemistry