4-[17BETA-METHOXY-17ALPHA-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-[17beta-methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by...

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Hauptverfasser: MUELLER UWE, BOHLMANN ULF, GRAWE DETLEF, HOESEL PETER, GLIESING SABINE, KNABE UWE, JACKE JURGEN, WEHMEIER DIETER, VOIGTLAENDER DAVID, MOSEBACH MICHAEL, MICHEL THOMAS, EILERS ROBERT, BAHL KLAUS, TILSTAM ULF, SANDER MICHAEL, GERECKE HAGEN, ERHART BERND
Format: Patent
Sprache:eng
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Zusammenfassung:The present invention relates to a method for the reliable and reproducible preparation of 4-[17beta-methoxy-17alpha-methoxymethyl-3-oxoestra-4,9-dien-11beta-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.).