Phosphoramidate Protides of Carbocyclic 2′, 3′??Dideoxy??2′, 3′??Didehydro??7??Deazaadenosine with Potent Activity Against HIV and HBV

…, R Hazen, LD Condreay, C McGuigan

Index: Gudmundsson, Kristjan S.; Wang, Zhicheng; Daluge, Susan M.; Johnson, Lance C.; Hazen, Richard; Condreay, Lynn D.; McGuigan, Christopher Nucleosides, Nucleotides and Nucleic Acids, 2004 , vol. 23, # 12 p. 1929 - 1937

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Citation Number: 10

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.