Copper-free click—a promising tool for pre-targeted PET imaging

Helen L. Evans; Rozanna L. Slade; Laurence Carroll; Graham Smith; Quang-De Nguyen; Lisa Iddon; Nazila Kamaly; Henning Stöckmann; Finian J. Leeper; Eric O. Aboagye; Alan C. Spivey

doi:10.1039/C1CC16220A

Copper-free click—a promising tool for pre-targeted PET imaging†

Helen L. Evans,^a Rozanna L. Slade,^a Laurence Carroll,*^a Graham Smith,^a Quang-De Nguyen,^a Lisa Iddon,^a Nazila Kamaly,^a Henning Stöckmann,^b Finian J. Leeper,^b Eric O. Aboagye^a and Alan C. Spivey^c

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^a Comprehensive Cancer Imaging Centre, Department of Surgery & Cancer, Hammersmith Campus, Imperial College, London, United Kingdom
E-mail: l.carroll@imperial.ac.uk
Tel: +44 (0)20 8383 3759

^b Department of Chemistry, University of Cambridge, Lensfield Road, Cambridge, UK

^c Department of Chemistry, Imperial College London, South Kensington Campus, London, UK

Abstract

The copper-free click (CFC) reaction has been evaluated for its potential application to in vivo pre-targeting for PET imaging. A promising biodistribution profile is demonstrated when employing [¹⁸F]2-fluoroethylazide ([¹⁸18F]1) and optimisation of the CFC reaction with a series of cyclooctynes shows that reactions proceed efficiently with tantalizing opportunities for application-specific tuning.

Chemical Communications

Copper-free click—a promising tool for pre-targeted PET imaging†

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Copper-free click—a promising tool for pre-targeted PET imaging

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