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.
(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.
Schoultz
B W
BW
Department of Chemistry, University of Oslo, Norway.
Arstad
E
E
Marton
J
J
Willoch
F
F
Drzezga
A
A
Wester
H-J
HJ
Henriksen
G
G