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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
Authors Info & Affiliations
, 1 , 5
Authors Info & Affiliations
The Open Medicinal Chemistry Journal
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16 July 2008 •
RESEARCH ARTICLE
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DOI: 10.2174/1874104500802010072
Abstract
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.
