- PROCESS FOR THE MANUFACTURE OF CIS(-)-LAMIVUDINE
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An improved process for the manufacture of Lamivudine. The process involves: (a) resolution of racemic lamivudine (intermediate of formula IX) to cis (±) lamivudine of formula (XII) by forming a crystalline salt and separating the product from an organic solvent by fractional crystallization; (b) resolution of cis (±) lamivudine to cis (?) isomer involving formation of S-Binol adduct of formula XIV.
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- 2-Substituted-4-substituted-1,3-dioxolanes and use thereof
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Nucleoside analogues containing a 1,3-dioxolane structure are suitable antiviral agents, particulary for the treatment of the HIV infections in mammals, especially humans. Examples of the nucleoside analogues include: cis-2-acetoxymethyl-4-(thymin-1′-yl)-1,3,-dioxolane, cis-2-hydroxymethyl-4-(thymin-1′-yl)-1,3-dioxolane, cis-2-benzoyloxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane, and cis-2-hydroxymethyl-4-(cytosin-1′-yl)-1,3-dioxolane. These compounds can be in the form of their racemates or their separate enantiomers.
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(2010/11/29)
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