Cyclo-Saligenyl-3′-Azido-2′,3′-Dideoxy- Thymidinemonophosphate (cycloSal-AZTMP) - A New Pro-Nucleotide Approach1 ?-

Abstract
The synthesis of cycloSal-AZTMPs 3a-h as new pro-nucleotides of AZTMP 2 is described. Phosphotriesters 3 selectively release AZTMP 2 by a controlled, chemically induced tandem reaction. CycloSal-AZTMPs 3 exhibited high biological activity in HIV-1/HIV-2 infected CEM/O cells but lost their activity nearly completely in CEM/TK- cells.