Synthesis of deoxydinucleoside phosphates containing 6-thio-substituted purine nucleobases

Abstract

An efficient preparative method to obtain, by the hydrogen phosphonate approach in solution, dinucleoside phosphates containing either 2′-deoxy-6-thioinosine or 2′-deoxy-6-thioguanosine at their 3′ end, as in compounds 6 and 7, is described. For this purpose appropriate 5′-OH-free sulfur-modified deoxynucleoside intermediates required for this synthesis have been defined, as exemplified with the case of 2′-deoxy-6-thioguanosine.