| abstract |
Inter alia, a process for the production of a nucleoside phosphorothioate derivative corresponding to the following general formula (I): <IMAGE> (I) characterized in that it comprises reacting a salt of a nucleoside H-phosphonate corresponding to the following general formula (II): <IMAGE> (II) with a thiol transfer agent corresponding to the following general formula (III):R2-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+ represents a suitable counter-cation; R1 represents an appropriate nucleoside or nucleoside analogue; R2 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. |