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@ARTICLE{Modemann:860016,
author = {Modemann, Daniel and Zlatopolskiy, Boris and Urusova,
Elizaveta and Zischler, Johannes and Craig, Austin and
Ermert, Johannes and Guliyev, Mehrab and Endepols, Heike and
Neumaier, Bernd},
title = {2-[18{F}]{F}luorophenylalanine: {S}ynthesis by
{N}ucleophilic 18{F}-{F}luorination and {P}reliminary
{B}iological {E}valuation},
journal = {Synthesis},
volume = {51},
number = {03},
issn = {1437-210X},
address = {Stuttgart [u.a.]},
publisher = {Thieme},
reportid = {FZJ-2019-00813},
pages = {664 - 676},
year = {2019},
abstract = {2-[18F]Fluorophenylalanine (2-[18F]FPhe), a promising PET
tracer for imaging of cerebral infarction and tumors, was
efficiently prepared from an easily accessible iodonium salt
precursor using Cu-mediated radiofluorination under “low
base” or “minimalist” conditions. Whereas significant
racemization was initially observed if the “minimalist”
protocol was applied for radiolabeling, it was completely
suppressed by the careful adjustment of 18F–
preprocessing. The initial biological study revealed a
higher uptake of 2- [18F]FPhe in different tumor cells in
comparison to that of [18F]FET. In contrast to 4-[18F]FPhe,
which suffered from rapid in vivo defluorination,
2-[18F]FPhe demonstrated a sufficient in vivo stability.
Conclusively, 2-[18F]FPhe is a promising PET probe which is
now readily available using Cu-mediated radiofluorination
under “minimalist” or “low base” conditions. The
simplicity of the translation of the proposed procedures to
automated synthesis modules allows a broad biological
evaluation of 2-[18F]FPhe. Notably, the novel protocol for
the preparation of N-Boc protected amino acids from the
respective Ni-Schiff base complexes was developed which
avoided application of strongly acidic conditions.},
cin = {INM-5},
ddc = {540},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {573 - Neuroimaging (POF3-573)},
pid = {G:(DE-HGF)POF3-573},
typ = {PUB:(DE-HGF)16},
UT = {WOS:000455805300005},
doi = {10.1055/s-0037-1611370},
url = {https://juser.fz-juelich.de/record/860016},
}