Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...
Patent
1990-12-05
1993-01-12
Shen, Cecilia
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitrogen attached directly or indirectly to the purine ring...
544180, 544215, 544264, 544265, 544276, 544277, 544309, 544312, 549214, 549358, 549397, 549449, 549453, C07D40504, C07D47300
Patent
active
051791048
ABSTRACT:
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 that 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.
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Chu Chung K.
Schinazi Raymond F.
Shen Cecilia
University of Georgia Research Foundation Inc.
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