Nucleoside phosphorothioate derivatives, synthesis and use thereof

Abstract

Inter alia, a process for the production of a nucleoside phosphorothioate derivative corresponding to the following general formula (I): ##STR1## characterized in that it comprises reacting a salt of a nucleoside H-phosphonate corresponding to the following general formula (II): ##STR2## with a thiol transfer agent corresponding to the following general formula (III): R.sup.2 --S--X (III) in the presence of a silylating agent and a base in a suitable solvent; and working-up the reaction mixture to isolate the desired product and change the counter-cation as desired; wherein M.sup.+ represents a suitable counter-cation; R.sup.1 represents an appropriate nucleoside or nucleoside analogue; R.sup.2 represents a desired protecting group, which may ultimately be removable by cleavage of its bond to the sulfur atom; and X represents a leaving group, is disclosed.

Dependencies are inferred from the claim text.