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1. IN4490/CHENP/2008 - NOVEL METHOD FOR THE PREPARATION OF STAVUDINE POLYMORPHIC FORM I AND FORM II

Office
Inde
Numéro de la demande 4490/CHENP/2008
Date de la demande 26.08.2008
Numéro de publication 4490/CHENP/2008
Date de publication 13.03.2009
Type de publication A
CIB
C07D 40/04
Déposants ARCHIMICA SRL
Inventeurs DI LERNIA, GIANLUCA
MANCINI, ALFREDO
MANCINI, FRANCO
VERGANI, DOMENICO
Données relatives à la priorité 102006901390325 28.02.2006 IT
Titre
(EN) NOVEL METHOD FOR THE PREPARATION OF STAVUDINE POLYMORPHIC FORM I AND FORM II
Abrégé
(EN)
A novel method for the preparation of stavudine polymorphic form I and form II is described; it's prepared starting from 5'-acetate-2',3'-diacetyl-5-methyluridine. The 5'-acetate-2',3'-diacetyl-5-methyluridine, by reaction with catalytic amounts of sodium methoxide in a C1-C4 alcholic solvent, gives crude stavudine form II. Crude stavudine form II, which doesn't need to be isolated or purified, can be converted into polymorphic form I by slurry at reflux is isopropanol.