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US 7,601,820 B2Granted
Preparation of alkyl-substituted 2-deoxy-2-fluoro-D-ribofuranosyl pyrimidines and purines and their derivatives
AssigneePharmasset, Inc.
InventorsPeiyuan Wang, Wojciech Stec, Byoung-Kwon Chun, Junxing Shi, Jinfa Du
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Abstract
The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.
Claims18
A compound of the following formula:
- wherein R3 and R5 can be independently H, CH3, benzyl, 4-methoxybenzyl, trityl, trialkylsilyl, t-butyldialkylsilyl, t-butyldiphenylsilyl, tetraisopropyldisilyl (TIPDS), tetrahydropyranyl (THP), methoxymethyl (MOM), β-methoxyethoxymethyl (MEM), or acyl;
- alternatively, R3 and R5 are linked through —SiR2—O—SiR2— or —SiR2—, wherein R is a lower alkyl.
Dependencies are inferred from the claim text.