método para preparar 4-[17 beta-metóxi-17alfa-metoximetil-3-oxoestra-4,9-diean- 11beta-il]benzaldeìdo (e)-oxima (asoprisnil)

• Main Authors: SABINE GLIESING, DIETER WEHMEIER, MICHAEL SANDER, DETLEF GRAWE, UWE KNABE, ROBERT EILERS, BERND ERHART, DAVID VOIGTLAENDER, UWE MUELLER, HAGEN GERECKE, JUERGEN JACKE, ULF BOHLMANN, MICHAEL MOSEBACH, THOMAS MICHEL, ULF TILSTAM, KLAUS BAHL, PETER HOESEL
• Format: Patent
• Language: Portuguese
• Published: 16.08.2011
• Subjects: 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

MéTODO PARA PREPARAR 4-[17BETA-METóXI-ALFA-METOXIMETIL-3-OXOESTRA-4,9-DIE N-11-BETA-ILIBENZALDEIDO (E)-OXIMA (ASOPRISNIL). A presente invenção refere-se a um método para preparação confiável e reprodutível de 4-[17beta-metóxi-17alfa-metoximetil-3-oxoestra4,9-dien-11beta-il]be nzaldeido (E)-oxima (asoprisnil) em escala-piloto e industrial. Asoprisnil, o qual é preparado por este método, é distinguido por uma estabilidade física muito boa e é, portanto, particularmente adequado para a fabricação de formas farmacêuticas sólidas (comprimidos, comprimidos revestidos, etc.). 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.).