AN AMORPHOUS FORM OF SOFOSBUVIR, A METHOD OF ITS PREPARATION AND ITS STABILIZATION

The invention relates to a preparation method of an amorphous form of sofosbuvir of formula I, (S)-isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4- fluoro-3-hydroxy-4-memyltetrahydrofuran-2-yl)methoxy)-(phenoxy)phosphorylamino)- propanoate, in particular aging of the a...

Full description

Saved in:
Bibliographic Details
Main Authors KREJCIK, Lukas, OBADALOVA, Iva
Format Patent
LanguageEnglish
French
Published 09.11.2017
Subjects
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
Online AccessGet full text

Cover

More Information
Summary:The invention relates to a preparation method of an amorphous form of sofosbuvir of formula I, (S)-isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4- fluoro-3-hydroxy-4-memyltetrahydrofuran-2-yl)methoxy)-(phenoxy)phosphorylamino)- propanoate, in particular aging of the amorphous form at a temperature of 0 to 90°C in an air environment with relative humidity of 0 to 50% RH for 1 to 90 days and its use in a drug form. L'invention concerne un procédé de préparation d'une forme amorphe de sofosbuvir de formule (I), (S)-isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-l(2H)-yl)-4- fluoro-3-hydroxy-4-méthyltétrahydrofuran-2-yl)méthoxy)-(phénoxy)phosphorylamino)-propanoate, en particulier le vieillissement de la forme amorphe à une température comprise entre 0 et 90 °C au sein d'un environnement d'air présentant une humidité relative comprise entre 0 et 50 % RH pendant 1 à 90 jours et son utilisation sous forme médicamenteuse.
Bibliography:Application Number: WO2017CZ00034