908337-67-7Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 2′-deoxy-2′, 2′-difluoro-5-halouridine phosphoramidate ProTides
Quintiliani, Maurizio,Persoons, Leentje,Solaroli, Nicola,Karlsson, Anna,Andrei, Graciela,Snoeck, Robert,Balzarini, Jan,McGuigan, Christopher
, p. 4338 - 4345 (2011/09/12)
We report the synthesis of a series of novel 2′-deoxy-2′, 2′-difluoro-5-halouridines and their corresponding phosphoramidate ProTides. All compounds were evaluated for antiviral activity and for cellular toxicity. Interestingly, 2′-deoxy-2′,2′-difluoro-5-iodo- and -5-bromo-uridines showed selective activity against feline herpes virus replication in cell culture due to a specific recognition (activation) by the virus-encoded thymidine kinase.
INTERMEDIATE AND PROCESS FOR PREPARING OF BETA- ANOMER ENRICHED 21DEOXY, 21 ,21-DIFLUORO-D-RIBOFURANOSYL NUCLEOSIDES
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Page/Page column 44, (2010/11/23)
A highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically acceptable slats thereof, in particular, the β- enriched anomer of gemcitabine hydrochloride of formula (lib) in purity of >99% is provided through utilization of a novel trichloroacetimidate of formula (I).
