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@PHDTHESIS{Humpert:878237,
author = {Humpert, Swen},
title = {{E}ntwicklung von {K}upplungsmethoden mit neuen
{M}arkierungsbausteinen zur {S}ynthese $^{18}${F}-markierter
{PSMA}-selektiver {L}iganden und argininreicher all-{D}
{P}eptide},
volume = {4425},
school = {Universität Köln},
type = {Dissertation},
address = {Jülich},
publisher = {Forschungszentrum Jülich GmbH Zentralbibliothek, Verlag},
reportid = {FZJ-2020-02706, Juel-4425},
series = {Berichte des Forschungszentrums Jülich},
pages = {VII, 160 S.},
year = {2020},
note = {Universität Köln, Diss., 2020},
abstract = {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. [...]},
cin = {INM-5},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {573 - Neuroimaging (POF3-573)},
pid = {G:(DE-HGF)POF3-573},
typ = {PUB:(DE-HGF)3 / PUB:(DE-HGF)11},
url = {https://juser.fz-juelich.de/record/878237},
}