Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 17, Pages 4996-4998Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.064
Keywords
Reboxetine; Stereoselective synthesis; SPECT; Imaging; Noradrenaline transporter
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Funding
- EPSRC
- Medical Research Scotland
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A stereoselective 10-step synthesis of iodophenoxy analogues of (2R,3S)-reboxetine has been developed with the aim of generating a new SPECT imaging agent for the noradrenaline transporter (NAT). In vitro testing of these compounds against various mono-amine transporters showed an ortho-iodophenoxy analogue to have excellent affinity (K-i 8.4 nM) and good selectivity for NAT. (C) 2009 Elsevier Ltd. All rights reserved.
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