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
نویسندگان
چکیده
(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.
منابع مشابه
[11C]GR103545: novel one-pot radiosynthesis with high specific activity.
INTRODUCTION GR103545 is a potent and selective kappa-opioid receptor agonist. Previous studies in non-human primates demonstrated favorable properties of [(11)C]GR103545 as a positron emission tomography tracer for in vivo imaging of cerebral kappa-opioid receptor. Nonetheless, advancement of [(11)C]GR103545 to imaging studies in humans was hampered by difficulties of its multiple-step radiosy...
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عنوان ژورنال:
دوره 2 شماره
صفحات -
تاریخ انتشار 2008