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Process for the preparation of Sofosbuvir

IP.com Disclosure Number: IPCOM000242199D
Publication Date: 2015-Jun-25
Document File: 3 page(s) / 186K

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Abstract

The present disclosure is to provide a novel process for the preparation of sofosbuvir of formula 1, using novel intermediates

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SOFOSBUVIR

The present disclosure relates to a process for the preparation of sofosbuvir. The present invention also relates to novel intermediates.

                                                                                                       

Nucleoside phosphoramidates are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

Sofosbuvir is chemically named as (S)-Isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2yl)methoxy)-(phenoxy)phosphorylamino)propanoate and is represented by the following chemical structure:

Formula 1

PROCESS FOR THE PREPARATION OF SOFOSBUVIR

The present disclosure is to provide a novel process for the preparation of sofosbuvir of formula 1, using novel intermediates of formula 9 and 10 as shown in below Scheme-I.

According to the present disclosure, compound of Formula-7a is reacted with a compound of formula 8a in the presence of a base to get a compound of Formula-9a; further reacting the compound of Formula-9 with uracil to get a compound of Formula-10; and deprotecting the compound of Formula-10 to get sofosbuvir of Formula-1 as shown in scheme-II


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