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Cyclam-based bifunctional ligands for selective metal ion complexation
Hörnerová, Alžběta ; Kotek, Jan (advisor) ; Havlíček, David (referee)
Recently, the increasing demand for targeting radiopharmaceuticals motiva- tes the research of bifunctional ligands which should be able to coordinate radiometal ion into a stable complex and also contains avalaible functional group for binding to a biological vector. Especially the wide range of copper radionuclides is sparking interest for potencial applications in diagnosis and therapy of tumorous diseases. The ligands of the cyclam family are one of the most suitable for Cu(II) complexation. Relatively small number of unsymmetrically trans-disubstituted derivates has been prepared be- cause of difficult and non-trivial synthesis of these compounds. In this Diploma thesis a new orthogonal protection of cyclam is presented as a possible route of preparation of these compounds. Through this intermediate a ligand with methylenephosphonate and methylene(p-aminobenzyl)phosphinate pendant arms was synthesized, copper complexes of the ligand were prepared and their isomerism and stability/inertness were studied. Keywords: PET, SPECT, radiotherapy, copper, bifunctional ligands, orthogonal pro- tection of cyclam. 1

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