Synthesis of two novel oxocyclam‐binding technetium complexes containing an analogue of cocaine

Abstract

International audienceIn order to visualize and quantify dopamine transporters, the synthesis of two novel ligands labelled with technetium-99 m (99mTc) has been investigated. A multi-step synthesis afforded two target ligands with a tropane skeleton and a macrocyclic complexing moiety. The choice and the position of substituents are in adequation with dopamine transporter structure. The radiolabelling of these ligands with 99mTc has been studied and the results make them good candidates for SPECT imaging

Full Control of the Regiospecific N-Functionalization of C-Functionalized Cyclam Bisaminal Derivatives and Application to the Synthesis of their TETA, TE2A, and CB-TE2A Analogues

“…However, this type of condensation requires long reaction times and often gives low yields . Another original way is the annelation reaction between an α,β-unsaturated ester and a linear tetraamine, with the pendant arm being provided either by the cyclizing reagent or by the polyamine . The idea of a template effect induced by rigidifying a linear tetraamine by condensation with a dicarbonyl compound followed by the cyclization of the resulting bisaminal with a biselectrophilic reagent emerged 20 years ago as a powerful synthetic tool for the synthesis of tetraazacycloalkanes and their selective N -functionalization .…”