A rapid synthesis of some 5′-amino- nucleosides and nucleotides as potential antiviral compounds

We describe a convenient method for the synthesis of 5′-amino-3′-azido-3′,5′-dideoxythymidine, and its conversion to a 5′-blocked phosphate derivative. The compounds are evaluated as inhibitors of HIV-1 in vitro, but prove to be poorly effective by comparison to their 5′-oxygen analogues.