Carbon-14 labeling of a trifluoromethoxy group: synthesis of a substance P antagonist

Synthesis of a carbon‐14 labeled trifluoromethoxy group has been accomplished using the stepwise oxidative fluorination–desulfurization of a readily prepared [14C]xanthate (5). This novel labeling procedure allowed a rapid synthesis of substance P antagonist candidate 1 that avoided potentially more...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 2001-10, Vol.44 (12), p.815-829
Hauptverfasser: Raab, Conrad E., Dean, Dennis C., Melillo, David G.
Format: Artikel
Sprache:eng
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Zusammenfassung:Synthesis of a carbon‐14 labeled trifluoromethoxy group has been accomplished using the stepwise oxidative fluorination–desulfurization of a readily prepared [14C]xanthate (5). This novel labeling procedure allowed a rapid synthesis of substance P antagonist candidate 1 that avoided potentially more complex ring‐labeling procedures. Similar procedures have been used to prepare C‐14 labeled trifluoromethyl and trifluoromethylamine groups. Copyright © 2001 John Wiley & Sons, Ltd.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.502