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  • Title: Phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine and related nucleosides with potent activity against HIV and HBV.
    Author: Gudmundsson KS, Daluge SM, Johnson LC, Jansen R, Hazen R, Condreay LD, McGuigan C.
    Journal: Nucleosides Nucleotides Nucleic Acids; 2003 Oct; 22(10):1953-61. PubMed ID: 14609234.
    Abstract:
    Syntheses of phosphoramidate protides of several 2',3'-dideoxy-3'-fluoroadenosine derivatives by treatment of the nucleoside with phosphorochloridates in the presence of pyridine and t-BuMgCl is described. Several of these protides showed significantly improved antiviral potency over the parent nucleoside against HIV and HBV. Especially marked was the improvement in potency of phosphoramidate protides of 2',3'-dideoxy-3'-fluoroadenosine against both HIV and HBV.
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