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-17alpha-ethynyl-17beta-hydroxy steroids by treatment with silyl-protected lithium acetylides followed by further desilylation. The resulting products are useful intermediates in the pr...

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Bibliographic Details
Main Authors SANDOVAL RODRIGUEZ CELSO MIGUEL, GUTIERREZ FUENTES LUIS GERARDO
Format Patent
LanguageChinese
English
Published 08.10.2014
Subjects
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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Summary:The invention relates to a process for ethynylating 16-methylene-17-keto steroids to the corresponding 16-methylene-17alpha-ethynyl-17beta-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.
Bibliography:Application Number: CN201280069059