The development of nucleoside pro-drugs capable of umdergoing intracellular activation to the corresponding nucleotides has become an area of intense interest. Nucleoside phosphoramidate to the monoesters are potent antiviral and/or anticancer agents with enhanced activity and reduced cytotoxicity. Likewise, nucleoside aryl phosphate monoesters can serve as ready pro-drug sources of free nucleosides and their 5’-monophosphates. In this work, we report a simple approach to stynthesize AZT/d4T phoshoramidate or aryl phosphate monoesters by Mg-cleavage 4-picolyl protected group. A typical process is depicted below.
