N. K. Jobson, A. R. Crawford, D. Dewar, S. L. Pimlott, A. Sutherland
1464-3405 (Electronic) 0960-894X (Linking)
Bioorg Med Chem Lett
WestCHEM, Department of Chemistry, University of Glasgow, Glasgow, UK.
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.