A 18F-labeled dibenzocyclooctyne (DBCO) derivative for copper-free click labeling of biomolecules

K. Kettenbach; T. L. Ross

doi:10.1039/C5MD00508F

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A ¹⁸F-labeled dibenzocyclooctyne (DBCO) derivative for copper-free click labeling of biomolecules†‡

K. Kettenbach

^a and T. L. Ross*^ab

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* Corresponding authors

^a Institute of Nuclear Chemistry, Johannes Gutenberg-University Mainz, Germany

^b Radiopharmaceutical Chemistry, Department of Nuclear Medicine, Hannover Medical School, 30625 Hannover, Germany
E-mail: ross.tobias@mh-hannover.de

Abstract

The new prosthetic group ¹⁸F-TEG-DBCO (dibenzocyclooctyne) can be prepared within a total reaction time of 60 min including purification with an overall yield (n.d.c.) of 34 ± 5%. Copper-free click cycloadditions with an azido-cRGD, a folate-azide and two α-MSH analogue azido-peptides resulted in very high RCYs and fast reaction kinetics.

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Article information

DOI: https://doi.org/10.1039/C5MD00508F
Article type: Research Article
Submitted: 03 Nov 2015
Accepted: 28 Dec 2015
First published: 12 Jan 2016
This article is Open Access

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Med. Chem. Commun., 2016,7, 654-657

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A ¹⁸F-labeled dibenzocyclooctyne (DBCO) derivative for copper-free click labeling of biomolecules

K. Kettenbach and T. L. Ross, Med. Chem. Commun., 2016, 7, 654 DOI: 10.1039/C5MD00508F

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