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

doi:10.2174/1874104500802010072

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

Open Med Chem J. 2008 Jul 16:2:72-4. doi: 10.2174/1874104500802010072.

Authors

B W Schoultz¹, E Arstad, J Marton, F Willoch, A Drzezga, H-J Wester, G Henriksen

Affiliation

¹ Department of Chemistry, University of Oslo, Norway.

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.