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Synthesis of 8-Methoxypenciclovir and 8-Methoxyganciclovir through Methyl Triflate, a New Potential Approach to Label Penciclovir and Ganciclovir with Carbon-11
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2003
Year
New CompoundsBioorganic ChemistrySynthetic VirologyMethylamine Salt PrecursorsMolecular BiologyOrganic ChemistryChemistryHeterocycle ChemistryChemical BiologyMedicinal ChemistryNew Potential ApproachMethyl TriflateVirologyPharmacologyAntiviral CompoundNatural Product SynthesisNatural SciencesMicrobiologyMedicineSynthetic ChemistryLabel Penciclovir
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.