PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS

The invention relates to a process for ethynylating 16-methylene-17-keto steroids to the corresponding 16-methylene-17a-ethynyl-17ß-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparati...

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Bibliographische Detailangaben
Hauptverfasser:	SANDOVAL RODRIGUEZ, CELSO MIGUEL, GUTIERREZ FUENTES, LUIS GERARDO
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	CHEMISTRY FOODS OR FOODSTUFFS FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BYSUBCLASSES A23B - A23J HUMAN NECESSITIES METALLURGY ORGANIC CHEMISTRY PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL STEROIDS THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OFNUTRITIVE QUALITIES, PHYSICAL TREATMENT THEIR TREATMENT, NOT COVERED BY OTHER CLASSES
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Beschreibung
Zusammenfassung:	The invention relates to a process for ethynylating 16-methylene-17-keto steroids to the corresponding 16-methylene-17a-ethynyl-17ß-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as e.g. Nestorone® or melengestrol acetate. L'invention concerne un procédé pour éthynyler des 16-méthylène-17-céto-stéroïdes en 16-méthylène-17a-éthynyl-17ß-hydroxy-stéroïdes correspondants par traitement avec des lithium-acétylides protégés par silyle suivi par désilylation ultérieure. Les produits résultants sont des intermédiaires utiles dans la préparation de plusieurs agents pharmaceutiquement actifs, tels que, par exemple, Nestorone® ou l'acétate de mélengestrol.