Abstract
In an effort to make HSV-tk gene reporter probes 8-FPCV and 8-FGCV labeled with fluorine-18,
via the nucleophilic substitution reaction of PCV and GCV quaternized methylamine
salt precursors with KF/Kryptofix 2.2.2, a new and unusual reaction through methyl
triflate was discovered. Subsequently, new compounds 8-MeOPCV and 8-MeOGCV were synthesized
from PCV and GCV in six steps with 12% and 20% overall chemical yield, respectively,
and a novel potential approach to label PCV and GCV with carbon-11 has been proposed.
Key words
gene reporter probes - herpes simplex virus thymidine kinase (HSV-tk) - positron emission
tomography (PET) - 8-methoxypenciclovir - 8-methoxyganciclovir
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