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Phosphoramidate protides of carbocyclic 2',3'-dideoxy-2',3'-didehydro-7-deazaadenosine with potent activity against
Kristjan S Gudmundsson1, Zhicheng Wang, Susan M Daluge
1Division of Chemistry, GlaxoSmithKline, Research Triangle Park, North Carolina, USA. Kristjan.S.Gudmundsson@gsk.com
Abstract:
Synthesis of phosphoramidate protides of carbocyclic D- and L-2',3'-dideoxy-2',3'-didehydro-7-deazaadenosine 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 nucleosides against both HIV and HBV.
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