Beyond azide–alkyne click reaction: easy access to 18F-labelled compounds via nitrile oxide cycloadditions

Boris D. Zlatopolskiy; René Kandler; Diana Kobus; Felix M. Mottaghy; Bernd Neumaier

doi:10.1039/C2CC31335A

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Beyond azide–alkyneclick reaction: easy access to ¹⁸F-labelled compounds vianitrile oxide cycloadditions†

Boris D. Zlatopolskiy,^ab René Kandler,^b Diana Kobus,^b Felix M. Mottaghy^ac and Bernd Neumaier*^b

Author affiliations

* Corresponding authors

^a Klinik für Nuklearmedizin, Aachen University, RWTH, Pauwelsstr. 30, 52074 Aachen, Germany

^b Max Planck Institute for Neurological Research, Gleueler Str. 50, 50931 Cologne, Germany
E-mail: bernd.neumaier@nf.mpg.de
Fax: +49-221-4726-298
Tel: +49-221-4726-270

^c Department of Nuclear Medicine, Maastricht University Medical Center, P. Debyelaan 25, 6229HX Maastricht, The Netherlands

Abstract

Radiofluorinated 4-fluorobenzonitrile oxide and N-hydroxy-4-fluorobenzimidoyl chloride rapidly react with different alkenes and alkynes under mild conditions. These cycloadditions are suitable for the preparation of low-molecular weight radiopharmaceuticals and, in a strain-promoted variant, can enable easy labelling of sensitive biopolymers.

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Article information

DOI: https://doi.org/10.1039/C2CC31335A
Article type: Communication
Submitted: 22 Feb 2012
Accepted: 17 Apr 2012
First published: 17 Apr 2012

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Chem. Commun., 2012,48, 7134-7136

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Beyond azide–alkyne click reaction: easy access to ¹⁸F-labelled compounds via nitrile oxide cycloadditions

B. D. Zlatopolskiy, R. Kandler, D. Kobus, F. M. Mottaghy and B. Neumaier, Chem. Commun., 2012, 48, 7134 DOI: 10.1039/C2CC31335A

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