Synthesis of Pyrimidine-Containing Nucleoside β-(R/S)-Hydroxyphosphonate Analogues

A concise route to nucleoside beta-hydroxyphosphonate analogues is described. The use of a nucleoside beta-ketophosphonate as the key intermediate allowed both the (R) and (S) isomers of beta-hydroxyphosphonate analogues in the pyrimidine series to be accessed. Such derivatives may be considered as stable mimics of 5'-monophosphate nucleosides and, therefore, could be the starting point for the development of potential therapeutic agents.