Synthesis and bioactivity of phosphorylated derivatives of stavudine

Abstract

KEYWORDSNovel phosphorylated derivatives of stavudine were synthesized by the reaction of bis(2chloroethyl)phosphoramidic dichloride/4-nitrophenyl phosphorodichloridate with various cyclic amines and amino acid esters in the presence of triethylamine in dry tetrahydrofuran through the corresponding monochloride intermediates 2a-l. Further reaction of the intermediates 2a-l with stavudine in tetrahydrofuran and pyridine in the presence of triethylamine formed the title compounds 4a-l. Their structures were cha…