A New Method for Radiosynthesis of 11C-Labeled Carbamate Groups and its Application for a Highly Efficient Synthesis of the Kappa-Opioid Receptor Tracer [11C]GR103545

B.W Schoultz1, E Årstad2, J Marton3, F Willoch4, A Drzezga5, H.-J Wester5, G Henriksen*, 1, 5
1 Department of Chemistry, University of Oslo, Norway
2 Institute of Nuclear Medicine, University College London Hospitals NHS Trust, 235 Euston Road, London NW1 2BU, UK; and Hammersmith Imanet Limited, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK
3 ABX Biomedizinische Forschungsreagenzien GmbH, Radeberg, Germany
4 Department of Radiology, Aker University Hospital, Aker Universitetssykehus HF, N-0514 Oslo, Norway
5 Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Germany

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© Schoultz et al.; Licensee Bentham Open.

open-access license: This is an open access article distributed under the terms of the Creative Commons Attribution License (, which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited.

* Address correspondence to this author at the Department of Nuclear Medicine, Klinikum rechts der Isar, Technische Universität München, Ismaningerstrasse 22, D-81675 München, Germany; Tel: +49 89 4149 2971; Fax: +49 89 4140 4841; E-mail:


11C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO2 and 11C-methylation reagents. [11C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding 11C-labeled carbamate groups in excellent yields under mild conditions (temperatures ≤ 40°C, 2 min reaction time). The utility of the method has been demonstrated by a highly efficient radiosynthesis of [11C]GR103545.