Process for the Preparation of Enantiomerically pure Beta-D-(-)-dioxolane-nucleosides

摘要

An asymmetric process for the preparation of enantiomerically pure beta -D-(-)-dioxolane-nucleosides. The enantiomerically pure dioxolane nucleosides are active HIV agents, that are significantly more effective than the prior prepared racemic mixtures of the nucleosides. The anti-viral activity of the compounds is surprising in light of the generally accepted theory that moieties in the endo conformation, including these dioxolanes, are not effective antiviral agents. The toxicity of the enantiomerically pure dioxolane nucleosides is lower than that of the racemic mixture of the nucleosides, because the nonnaturally occurring alpha -isomer is not included. The product can be used as a research tool to study the inhibition of HIV in vitro or can be administered in a pharmaceutical composition to inhibit the growth of HIV in vivo. <IMAGE> <IMAGE>