ETD

• Actinium
• alphaimmunotherapy
• N-nitroso

This thesis is devoted to the synthesis of new chelating agents for actinium and actnoids (An), as part of a research effort to the production of new radio immune drugs.

The first part is dedicated to the synthesis of the first member of a brand new class of An chelating agents based on dendrimers. These compounds are particular interesting because they can give drugs with an higher dose load (i.e. with more than one An atom bound by the same chelating agent), extremely difficult to be realized with traditional methodology. The identified target molecule is benzoyl-(Glu)G3-OEt a dendrimer of glutamic acid.

The second part is dedicated to the synthesis of new nitrogenated chelating agents. New synthetic ways for the synthesis of N-nitroso compounds are inspected. These species have been chosen by using one of the synergic strategies nowadays so widely recommended in industrial management manuals. In fact their complexing properties toward transition metals and lanthanoids are well known and it is of scientific and applicative interest to synthesize new suitable chelating agents to make possible the study of their chelating affinity towards An. At the same time, they can be used as both starting material for the synthesis of hydrazinic chelating agents and synthetic scaffolds for the synthesis of a wide range of pendant-type-macrocyclic bifunctionalised chelating agents.

The third part is dedicated to the identification of new synthetic pathway towards classical pendant-type macrocyclic bifunctionalised chelating agents.