Approaches to functionalised amine-based ligands for radiopharmaceutical delivery systems

Abstract

This thesis describes the results of an investigation into the synthesis and behaviour of tetra-aza ligands intended for use as novel diagnostic radiopharmaceutical agents through technetium complexation and attachment to bioactive targeting groups.  The literature concerning radiopharmaceutical imaging agents is reviewed.  The main body of the thesis concerns a study focused on two ligand classes, the 1,4,8,11-tetraazaundecanes (TAs) and 3,3,9,9-tetramethyl-4,8-diazaundecane-2,10-dione dioximes (propylene amine oximes; PnAOs), in which a single arylmethyl substituent is attached at the apical position (C-6), either directly or via an ether-linkage.  A number of routes have been explored to TA-derivatives bearing a benzyl or 4-borombenzyl group and bis-oxo-TA derivatives have been successfully prepared.  However, conversion of these into their saturated analogues has proved difficult.

Methods for the attachment of sulfonamide substituents to the arylmethyl side-arm have also been developed.

In a parallel study, three novel oxotechnetium(V) complexes of analogous apically substituted PnAO derivatives have been prepared and characterised by single-crystal X-ray diffraction.  Comparison of the structures of these complexes with literature data an the results of recent structural studies of other transition metal-ion complexes with such ligands gives useful insight into both the effect of apical substitution and the ability of other metal ions to ‘mimic’ the Tc-O core.

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