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Synthesis of phosphono-bis(phosphinate) cyclam derivative
Chrappa, Michal ; Hermann, Petr (advisor) ; Veselý, Jan (referee)
Radiopharmaceuticals containing copper isotopes can be used as diagnostic tools (methods PET, SPECT) or agents for tumour treatment. Copper radionuclides must be applied into the organism in the form of a coordination compound with suitable ligand. Derivatives of 1,4,8,11-tetraazacyclotetradecane (cyclam) are some of the most suitable ligands for Cu (II). A coordination compound must be thermodynamically stable and kinetically inert, the ligand must coordinate the metal ion as quickly as possible. In this Diploma thesis, one of the first unsymmetrically substituted derivatives of cyclam has been synthesized using two methods of orthogonal protection. The synthesized ligand contains one phosphonate and one methylene bis(phosphinate) pendant arm. Copper complex of the ligand was prepared, and its acid assisted dissociation kinetics were studied.
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Synthesis of asymetrically substituted derivatives of cyclam
Chrappa, Michal ; Hermann, Petr (advisor) ; Kubíček, Vojtěch (referee)
Copper radionuclides have a potential in nuclear medicine as diagnostic or therapeutic agents. Copper isotopes are used in the form of coordination compounds with various ligands, such as derivatives of 1,4,8,11-tetraazacyclotetradecane (cyclam). Properties of such complexes can be modified by pendant arms introduced on amino groups of cyclam. This thesis is aimed on the synthesis of asymmetrically substituted cyclam derivative with derivatives of phosphorous acids in 1,8- position. In spite of the fact, that the target ligand has not been successfully synthesised, various possibilities of substitution on diprotected cyclam were investigated. New possibilities of orthogonal protection of cyclam were found as well. Keywords: PET, SPECT, copper complexes, cyclam protection, phosphonic acids
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Macrocyclic ligands for selective complexation of large cations
Šefčík, Martin ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
4 Abstract Nowadays, macrocyclic complexes of actinides receive an increasing attention for their potential applications in radiotherapy. It requires significant demands on their thermodynamic and kinetic stability which are particularly influenced by an appropriate choice of a ligand. This Thesis focuses on a synthesis and characterization of two ligands that are potentially applicable for complexation of lanthanum as a model of radioactive actinium. Both ligands are based on a fifteen-membered cycle containing pyridine group, 15-pyN3O2. The first ligand, H4L1, contains two phosphonate pendant arms. The second ligand, H2L2, contains two phosphinate pendant arms. Both compounds were prepared and characterized. Keywords Macrocyclic ligands, large cations, phosphonic acids, phosphinic acids, dissociation constants
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