Design and synthesis of (2 R,3 S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter

Abstract

A stereoselective 10-step synthesis of iodophenoxy analogues of (2 R,3 S)-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.