The traceless Staudinger ligation for indirect 18F-radiolabelling

Laurence Carroll; Sophie Boldon; Romain Bejot; Jane E. Moore; Jérôme Declerck; Véronique Gouverneur

doi:10.1039/C0OB00564A

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The traceless Staudinger ligation for indirect ¹⁸F-radiolabelling†‡

Laurence Carroll,^a Sophie Boldon,^a Romain Bejot,^a Jane E. Moore,^b Jérôme Declerck^c and Véronique Gouverneur*^a

Author affiliations

* Corresponding authors

^a University of Oxford, Chemistry Research Laboratory, Mansfield Road, Oxford, UK
E-mail: veronique.gouverneur@chem.ox.ac.uk

^b AstraZeneca UK, Alderley Park, Cheshire, UK

^c Siemens Molecular Imaging, 23–38 Hythe Bridge Street, Oxford, UK

Abstract

The Staudinger ligation of phosphine-substituted thioesters with ¹⁸F-fluoroethylazide has been successfully applied to access ¹⁸F-labelled molecules in radiochemical yields superior to 95%; the first fluorous variant of a Staudinger radio-ligation has been validated.

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Article information

DOI: https://doi.org/10.1039/C0OB00564A
Article type: Paper
Submitted: 10 Aug 2010
Accepted: 06 Oct 2010
First published: 22 Nov 2010

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Org. Biomol. Chem., 2011,9, 136-140

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The traceless Staudinger ligation for indirect ¹⁸F-radiolabelling

L. Carroll, S. Boldon, R. Bejot, J. E. Moore, J. Declerck and V. Gouverneur, Org. Biomol. Chem., 2011, 9, 136 DOI: 10.1039/C0OB00564A

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Organic & Biomolecular Chemistry