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
Identifiers and Pagination:Year: 2008
First Page: 72
Last Page: 74
Publisher Id: TOMCJ-2-72
Article History:Received Date: 28/5/2008
Revision Received Date: 1/7/2008
Acceptance Date: 1/7/2008
Electronic publication date: 16/7/2008
Collection year: 2008
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.
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.