Preparation of alkyl-substituted 2-deoxy-2-fluoro-D-ribofuranosyl pyrimidines and purines and their derivatives
First Claim
Patent Images
1. A 3,5-di-O-protected-2-deoxy-2-fluoro-2-C-methyl-D-ribono-γ
- -lactone of the following general formula;
4 Assignments
0 Petitions
Accused Products
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-o-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.
-
Citations
18 Claims
-
1. A 3,5-di-O-protected-2-deoxy-2-fluoro-2-C-methyl-D-ribono-γ
- -lactone of the following general formula;
- View Dependent Claims (2, 3, 4, 5, 14, 15)
- -lactone of the following general formula;
-
6. A process for the preparation of a lactone intermediate, 46,
-
7. A process of preparing a 2′
- -deoxy-2′
-fluoro-2′
-C-methyl-β
-D-ribofuranosyl nucleoside of the following formula;
- View Dependent Claims (8, 9, 10)
- -deoxy-2′
-
11. A process for the preparation of a 2′
- -deoxy-2′
-fluoro-2′
-C-methyl-β
-D-ribofuranosyl nucleoside of formula 63
- -deoxy-2′
-
12. A process for the preparation of a 2′
- -deoxy-2′
-fluoro-2′
-C-methyl-β
-D-ribofuranosyl nucleoside of formula 14
- -deoxy-2′
-
13. A process for the preparation of a 2′
- -deoxy-2′
-fluoro-2′
-C-methyl-β
-D-ribofuranosyl nucleoside of formula 14,
- -deoxy-2′
- 16. A 2-alkyl-4,5-di-O-protected-2,3-dihydroxy-pentanoic-acid ester of the following general formula:
-
18. A process for the preparation of the diol of the formula,
Specification