Process for preparing entecavir and intermediates thereof

Process for preparing entecavir and intermediates thereof

It comprises the preparation of entecavir of formula (I), or a pharmaceutically acceptable salt thereof, or a hydrate thereof by submitting a compound of formula (III) where X is an halogen selected from Cl, Br, and I, first to a hydrolysis reaction using formic acid and then to a deprotection react...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: BERENGUER MAIMO, RAMON, BADIA PEREZ, LAURA, ARIZA PIQUER, JAVIER, VELASCO TURBAU, JAVIER, GASANZ GUILLEN, YOLANDA
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:It comprises the preparation of entecavir of formula (I), or a pharmaceutically acceptable salt thereof, or a hydrate thereof by submitting a compound of formula (III) where X is an halogen selected from Cl, Br, and I, first to a hydrolysis reaction using formic acid and then to a deprotection reaction, and isolating the entecavir either as free base or as a pharmaceutically acceptable salt. It also comprises intermediates which intervene in this preparation process.