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Complexes of 1,4,7-triazacyclononane phosphinate derivatives
Lebruška, Viktor ; Kubíček, Vojtěch (advisor) ; Štěpnička, Petr (referee)
Phosphorus pendant arms accelerate the complexation of gallium(III) ions with macrocyclic chelators, which is crucial parameter in labelling by the radioisotope 68 Ga and their use in positron emission tomography (PET). In this thesis, new chelators for the selective complexation of gallium(III) ions were designed. Two chelators derived from the TACN macrocycle were prepared, namely: 1,4,7-triazacyclononane-1-methyl-methylene- bis(phosphinic) acid (H2L1 ) and 1,4,7-triazacyclononane-1-methyl-methylene- bis(phosphinato)-4,7-bis(methyl-phosphinic) (H4L2 ). The acidobase properties of the H2L1 were investigated using potentiometric and NMR titrations. Complexes of H2L1 with Ni(II), Cu(II), Zn(II) and Ga(III) were investigated using potentiometric titrations, which showed the high stability of these complexes. The solid-state structures of the Cu-L1 and Zn-L1 complexes were determined by X-ray diffraction. Complexation of the radioisotope 68 Ga(III) was studied for chelators H2L1 , H4L2 and for several related chelators with phosphorus pendant arms. The complexation study showed that chelators with the methylene-bis(phosphinate) pendant arm and some other phosphorus chelators derived from the TACN macrocycle accelerate complexation of gallium(III) ions. Using Dynamic PET scanning and ex-vivo...
Dipicolylamine modified with a bis(phosphinate) group
Jaroš, Adam ; Kubíček, Vojtěch (advisor) ; Matulková, Irena (referee)
Ligand DPABPin was synthesized by Mannich reaction. Acid-base properties of the ligand were studied by potentiometric titrations. Protonation constants and stability constants of complexes with Cu2+ , Zn2+ and Ni2+ were determined. Cu2+ and Ni2+ complexes were isolated and their geometry was determined using X-Ray diffraction analysis.
Polydentate aminodiphosphinates
Böhmová, Zuzana ; Kubíček, Vojtěch (advisor) ; Vojtíšek, Pavel (referee)
Two linear aminodiphosphinates (H3L1 , H5L2 ) and one cyclic aminodiphosphinate (H2L3 ) were prepared and studied. Newly prepared compounds were characterized by NMR, MS and EA (elemental analysis). Acid-base and coordination properties of ligands were studied. Protonation constants and stability constants of complexes with Zn2+ , Ni2+ and Cu2+ metal ions were determined by potentiometry. Keywords Ligands, dissociation constants, potentiometry, phosphinates, complexes.
Phosphonate and phosphinate derivatives of dipicolylamine
Hlinová, Veronika
The Diploma Thesis deals with preparation of one phoshonate and two phospinate derivatives of dipicolylamine. Dissociation constants of prepared ligands were determined by potentiometric and NMR titration. Coordination properties of the compounds were studied by combination of potentiometry and UV-VIS spectrophotometry. Stability constants of complexes with selected transition metal ions (Cu2+ , Ni2+ a Zn2+ ) and alkali-earth metals ions (Ca2+ , Mg2+ ) were calculated. Acid-base and coordination properties in the solid state were studied by X-ray diffraction on single-crystals.
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
Complexes of polydentate ligands
Sedláčková, Simona ; Kubíček, Vojtěch (advisor) ; Kotek, Jan (referee)
Polydentate ligands are useful in many industries, mainly because of their ability to form complexes. The aim of this thesis is to study acid-base and coordination properties of polydentate ligands from the group of polyaminopolyphosphonates DTPMP and HMDTMP. The protonation constants of ligands as well as stability constants of complexes with biologically relevant ions Cu2+ , Zn2+ , Ni2+ , Mg2+ , Ca2+ , Co2+ , K+ and Na+ were determined by potentiometric titration. 31 P-NMR titration was used to determine pKa on nitrogen atoms, which could not be measured by potenciometric titration. Seven pKa for HMDTMP ligand and nine for DTPMP were obtained. The stability constants show that the HMDTMP ligand forms less stable complexes than the DTPMP ligand.
Complexes of 1,4,7-triazacyclonane for nuclear medicine
Lebruška, Viktor ; Kubíček, Vojtěch (advisor) ; Schulz, Jiří (referee)
The use of metal isotopes for the study of tissues in the field of nuclear medicine is currently being developed. Metal isotopes are accumulated non-specifically in the body. Therefore, it is necessary for diagnosis and therapy to use suitable ligands, which form a thermodynamically stable and kinetically inert complex with the given metal ion, which can be attached to a suitable targeting group. Isotopes of gallium and copper are suitable for imaging od therapy. The cavity of the 1,4,7-triazacyclononane is suitable for the complexation of gallium, copper and some other metals with a small radius. However, the macrocycle itself does not form thermodynamically stable complexes, so the nitrogen atoms must be substituted by proper pendant arms, such as carboxylates. In recent years organic residues of phosphoric acids are also used. This work deals with substances that are derivatives of 1,4,7-triazacyclononane and contain phosphorus arms, which were studied in recent years. Keywords complexes, ligands, dissociation constants, stability constants
Phosphonate and phosphinate derivatives of dipicolylamine
Hlinová, Veronika
The Diploma Thesis deals with preparation of one phoshonate and two phospinate derivatives of dipicolylamine. Dissociation constants of prepared ligands were determined by potentiometric and NMR titration. Coordination properties of the compounds were studied by combination of potentiometry and UV-VIS spectrophotometry. Stability constants of complexes with selected transition metal ions (Cu2+ , Ni2+ a Zn2+ ) and alkali-earth metals ions (Ca2+ , Mg2+ ) were calculated. Acid-base and coordination properties in the solid state were studied by X-ray diffraction on single-crystals.
Phosphonate and phosphinate derivatives of dipicolylamine
Hlinová, Veronika ; Kubíček, Vojtěch (advisor) ; Vojtíšek, Pavel (referee)
The Diploma Thesis deals with preparation of one phoshonate and two phospinate derivatives of dipicolylamine. Dissociation constants of prepared ligands were determined by potentiometric and NMR titration. Coordination properties of the compounds were studied by combination of potentiometry and UV-VIS spectrophotometry. Stability constants of complexes with selected transition metal ions (Cu2+ , Ni2+ a Zn2+ ) and alkali-earth metals ions (Ca2+ , Mg2+ ) were calculated. Acid-base and coordination properties in the solid state were studied by X-ray diffraction on single-crystals.

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