METHOD FOR PREPARING 4-[17β-METHOXY-17α-METHOXYMETHYL-3-OXOESTR A-4,9-DIEN-11β-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL)

METHOD FOR PREPARING 4-[17β-METHOXY-17α-METHOXYMETHYL-3-OXOESTR A-4,9-DIEN-11β-YL]BENZALDEHYDE (E)-OXIME (ASOPRISNIL)

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

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Bibliographische Detailangaben
Hauptverfasser: SABINE GLIESING, DIETER WEHMEIER, MICHAEL SANDER, DETLEF GRAWE, UWE KNABE, ROBERT EILERS, BERND ERHART, DAVID VOIGTLAENDER, UWE MUELLER, HAGEN GERECKE, ULF BOHLMANN, MICHAEL MOSEBACH, THOMAS MICHEL, ULF TILSTAM, JUERGEN JACKEN, KLAUS BAHL, PETER HOESEL
Format: Patent
Sprache:eng ; spa
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-[17β-methoxy-17α-methoxymethyl-3-oxoestra-4,9-dien-llβ- 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.). La presente invención se relaciona con un método para la preparación confiable y reproducible de (E)-oxima de 4-[17ß-metoxi-1 7a-metoximetil-3-oxoestra-4,9-dien-11ß-il]benzalde hído (asoprisnil) a escala piloto y de fabricación. El asoprisnil que se prepara con este método se distingue por una estabilidad física muy buena, por lo que es particularmente apropiado para la fabricación de formas farmacéuticas sólidas (tabletas, tabletas recubiertas, etcétera).