METHOD FOR PREPARING 4-[17.BETA.-METHOXY-17.ALPHA.-METHOXYMETHYL-3-OXOESTRA-4,9-DIEN-11.BETA.-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL)

METHOD FOR PREPARING 4-[17.BETA.-METHOXY-17.ALPHA.-METHOXYMETHYL-3-OXOESTRA-4,9-DIEN-11.BETA.-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL)

The present invention relates to a method for the reliable and reproducible preparation of 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-ll.beta.- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distingui...

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Hauptverfasser: VOIGTLAENDER, DAVID, MOSEBACH, MICHAEL, GERECKE, HAGEN, EILERS, ROBERT, KNABE, UWE, TILSTAM, ULF, JACKE, JUERGEN, GLIESING, SABINE, WEHMEIER, DIETER, BOHLMANN, ULF, MUELLER, UWE, HOESEL, PETER, MICHEL, THOMAS, BAHL, KLAUS, SANDER, MICHAEL, GRAWE, DETLEF, ERHART, BERND
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
STEROIDS
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Zusammenfassung:The present invention relates to a method for the reliable and reproducible preparation of 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-ll.beta.- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.). L'invention porte sur une méthode de préparation de 4-[17.beta.-methoxy-17.alpha.-méthoxyméthyl-3-oxoestra-4,9-dien-11.beta.-yl]benzaldéhyde (e)-oxime (asoprisnil) à l'échelle pilote et à l'échelle de fabrication. L'asoprisnil, préparé par cette méthode, qui se distingue par une très bonne stabilité physique, est donc particulièrement adapté à la fabrication de formes pharmaceutiques solides (comprimés, comprimés pelliculés, etc.).