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 (http://creativecommons.org/licenses/by/2.5/), 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: G.Henriksen@lrz.tum.de


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.