TY  - THES
AU  - Humpert, Swen
TI  - Entwicklung von Kupplungsmethoden mit neuen Markierungsbausteinen zur Synthese $^{18}$F-markierter PSMA-selektiver Liganden und argininreicher all-D Peptide
VL  - 4425
IS  - Juel-4425
PB  - Universität Köln
VL  - Dissertation
CY  - Jülich
M1  - FZJ-2020-02706
M1  - Juel-4425
T2  - Berichte des Forschungszentrums Jülich
SP  - VII, 160 S.
PY  - 2020
N1  - Universität Köln, Diss., 2020
AB  - Positron emission tomography (PET) is an indispensable tool in clinical research and diagnostics for the visualization of physiological and pathophysiological processes at themolecular level $\textit{in vivo}$. For different clinical examinations, PET requires radiolabeled, tailormade molecules, so called radiotracers, specifically targeting selected molecular structures. The development and efficient production of these tracers is therefore an essential task in PETresearch. Direct radiolabeling approaches with $^{18}$F, one of the most suitable radionuclides for PET, require harsh reaction conditions and are often not applicable for sensitive biomolecules. However, indirect methods using radiolabeled building blocks are well suited as alternatives although they are more time consuming due to multi step syntheses and thus less effective. The aim of this work was the further development and application of novel indirect radiolabeling methods for peptides. Accordingly, two different peptides have been used for radiolabeling. Radiolabeled PSMA-selective ligands and arginine-rich, fully D-enantiomeric peptides (D3 and RD2) should be prepared in this work. PSMA-selective peptidomimetics are currently being used for the detection of prostate carcinoma and the D-enantiomeric peptides in Alzheimer's research since they potentially enable a causal treatment of this disease which is otherwise not possible so far. For the conjugation of the promising synthon (Z)-2-[$^{18}$F]fluorohex-1-en-1-yl(phenyl)iodoniumtosylate ([$^{18}$F]FHexI$^{+}$), various Pd-catalyzed cross-coupling reactions were first investigated using structurally simple coupling partners. After radiosynthesis of [$^{18}$F]FHexI$^{+}$ under aqueous conditions starting from [$^{18}$F]fluoride, subsequently both, the Sonogashira coupling and the Suzuki coupling reaction were carried out as a one-pot reaction directly in the initial labelling mixture. [...]
LB  - PUB:(DE-HGF)3 ; PUB:(DE-HGF)11
UR  - https://juser.fz-juelich.de/record/878237
ER  -