C. Meier et al., ,3'-DIDEOXY-2',3'-DIDEHYDROYTHYMIDINEMONOPHOSPHATE (CYCLOSAL-D4TMP) -A NEW PRO-NUCLEOTIDE APPROACH, Nucleosides & nucleotides, 16(7-9), 1997, pp. 1303-1306
The synthesis of cycloSal-d4TMP 3a-g as new pro-nucleotide approach fo
r d4TMP 2 is described. Phosphotriesters 3 release the d4TMP 2 selecti
vely by a controlled, chemically induced tandem reaction. CycloSal-pho
sphotriesters 3 exhibited high biological activity against HIV-1/HIV-2
in CEM cells which was completely retained in CEM TK- cells.