Process for alkynylating 16-substituted-17-keto steroids

Process for alkynylating 16-substituted-17-keto steroids

A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17[alpha]-ethynyl-17[beta]-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the preparation of several pharm...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: SANDOVAL RODRIGUEZ CELSO MIGUEL, GUTIERREZ FUENTES LUIS GERARDO
Format: Patent
Sprache:chi ; eng
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:A process ethynylates 16-methylene-17-keto steroids to the corresponding 16-methylene-17[alpha]-ethynyl-17[beta]-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 TM or melengestrol acetate. 本发明涉及种通过使用甲硅烷基保护的锂乙炔化物处理、然后进步脱甲硅烷基化而将16-亚甲基-17-酮基类固醇乙炔基化为相应的16-亚甲基-17α-乙炔基-17β-羟基类固醇的方法。所获得的产物可用作为制备数种制药学活性试剂的中间体，例如Nestorone®或醋酸美仑孕酮。