A New Method for Radiosynthesis of C-Labeled Carbamate Groups and its Application for a Highly Efficient Synthesis of the Kappa-Opioid Receptor Tracer [C]GR103545.
B W Schoultz, E Arstad, J Marton, F Willoch, A Drzezga, H-J Wester, G Henriksen
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引用次数: 14
Abstract
(11)C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO(2) and (11)C-methylation reagents. [(11)C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding (11)C-labeled carbamate groups in excellent yields under mild conditions (temperatures = 40 degrees C, 2 min reaction time). The utility of the method has been demonstrated by a highly efficient radiosynthesis of [(11)C]GR103545.