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3. 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

Author

Schoultz, B.W, Årstad, E, Marton, J, Willoch, F, Drzezga, A, Wester, H.-J, and Henriksen, G

Abstract

C-labeled carbamates can be obtained in a three-component coupling reaction of primary or secondary amines with CO and C-methylation reagents. [C]Methyl-triflate mediated methylation of carbamino adducts provides the corresponding C-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 [C]GR103545.

Published
2008

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