Process for the preparation of sofosbuvir
AssigneeOptimus Drugs (P) Limited
InventorsSrinivas Reddy Desi Reddy, Srinivas Rao Velivela
Life of this patent
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Abstract
The present invention relates to an improved, commercially viable and industrially advantageous process for the preparation of sofosbuvir, which uses reagents that are less expensive and easier to handle.
Claims18
A process for the preparation of sofosbuvir of formula (I) comprising the step of reacting a compound of formula (III), 2′-deoxy-2′-fluoro-2′-C-methyluridine, with a compound of formula (II), (S)-isopropyl-2-(((R)-[(2,3,4,5,6-pentafluoro-phenoxy-phosphorylamino]propanoate, in the presence of a metallic salt, optionally further in the presence of a base and a solvent, to obtain sofosbuvir of formula (I)
A process for the preparation of sofosbuvir of formula (I) comprising the steps of
- (a) deprotecting N4,3′,5′-tribenzoyl-2′-deoxy-2′-fluoro-2′-C-methylcytidine of formula (V) in the presence of an acid to obtain 3′,5′-dibenzoyl-2′-deoxy-2′-fluoro-2′-C-methyluridine of formula (IV)
- (b) hydrolyzing the 3′,5′-dibenzoyl-2′-deoxy-2′-fluoro-2′-C-methyluridine of formula (IV) in the presence of a base and a solvent to obtain 2′-deoxy-2′-fluoro-2′-C-methyluridine of formula (III)
- and
- (c) reacting the 2′-deoxy-2′-fluoro-2′-C-methyluridine of formula (III) with (S)-isopropyl-2-(((R)-[(2,3,4,5,6-pentafluoro-phenoxy-phosphorylamino]propanoate of formula (II) in the presence of a metallic salt, optionally further in the presence of a base and a solvent, to obtain sofosbuvir of formula (I)
Dependencies are inferred from the claim text.