Method for preparing 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyde (E)-oxime (asoprisnil)

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

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Hauptverfasser: SABINE GLIESING, MICHAEL SANDER, DIETER WEHMEIER, DETLEF GRAWE, UWE KNABE, ROBERT EILERS, DAVID VOIGTLAENDER, BERND ERHART, UWE MUELLER, HAGEN GERECKE, JUERGEN JACKE, ULF BOHLMANN, MICHAEL MOSEBACH, THOMAS MICHEL, ULF TILSTAM, KLAUS BAHL, PETER HOESEL
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to a method for the reliable and reproducible preparation of 4-[17ß-methoxy-17a-methoxymethyl-3-oxoestra-4,9-dien-llß- 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.).