Diastereoselective synthesis of polyfunctionalized piperidines as precursors of dopamine transporter imaging agents

The design and synthesis of a new kind of precursors of radiolabelled tracer agents for dopamine transporters imaging is described. The concept is based on the possibility of introducing the radioelement far from the sites of recognition and on the fact that only the labelled marker could cross the blood brain barrier to reach the dopamine transporters. For this purpose, a polyfunctionalized piperidine was synthesized bearing two aldehyde functions in the configuration allowing the formation of a tropane analog after the introduction of complexing moieties and complexation of a radioactive metal.