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US 2004/0176587 A1Published application
Process for the preparation of l-ribavirin
AssigneeArchimica GmbH
InventorsAldo Banfi, Bruno Dall'Oro, Marco Frigerio, Alfredo Mancini
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Abstract
A process for the preparation of L-ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid and of a solvent. Said process comprises: a) the reaction of a triazole of formula (I) with a protected L-ribofuranose of formula (II)b) the removal of the Pg groups and, optionally, the conversion into a carboxyamide group of the R2 group of the compound obtained of formula (III) to give L-ribavirin. 1
Claims10
A process for the preparation of L-ribavirin which comprises:
- a) the reaction of a triazole of formula
- 9
- wherein r2 represents a C1-C4 alkoxycarbonyl, arylalkoxycarbonyl, carboxy, cyano, carboxyamide group with a protected l-ribofuranose of formula
- 10
- wherein Pg represents a group protecting the hydroxyl function and R1 represents a leaving group selected from among C1-C4 acyloxy, aryloxy and halogen;
- in the presence of a Lewis acid (IV) and of a solvent;
- and
- b) the removal of the Pg groups and, optionally, the conversion of the R2 group of the compound obtained of formula
- 11
- wherein Pg and R2 have the meanings given above, into a carboxyamide group, to give L-ribavirin:
7 more elements
Dependencies are inferred from the claim text.