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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| creator | SANDOVAL RODRIGUEZ, CELSO MIGUEL GUTIERREZ FUENTES, LUIS GERARDO |
| description | 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. |
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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.</description><language>eng ; fre</language><subject>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</subject><creationdate>2020</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20200915&DB=EPODOC&CC=CA&NR=2859852C$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20200915&DB=EPODOC&CC=CA&NR=2859852C$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>SANDOVAL RODRIGUEZ, CELSO MIGUEL</creatorcontrib><creatorcontrib>GUTIERREZ FUENTES, LUIS GERARDO</creatorcontrib><title>PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS</title><description>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.</description><subject>CHEMISTRY</subject><subject>FOODS OR FOODSTUFFS</subject><subject>FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BYSUBCLASSES A23B - A23J</subject><subject>HUMAN NECESSITIES</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL</subject><subject>STEROIDS</subject><subject>THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OFNUTRITIVE QUALITIES, PHYSICAL TREATMENT</subject><subject>THEIR TREATMENT, NOT COVERED BY OTHER CLASSES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2020</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLAICPJ3dg0OVnDzD1Jw9PGO9Iv0cQzx9HNXMDTTDQ51Cg7xDAkNcXXRNTTX9XYN8VcIDnEN8vd0CeZhYE1LzClO5YXS3Azybq4hzh66qQX58anFBYnJqXmpJfHOjkYWppYWpkbOxoRVAADW3CfG</recordid><startdate>20200915</startdate><enddate>20200915</enddate><creator>SANDOVAL RODRIGUEZ, CELSO MIGUEL</creator><creator>GUTIERREZ FUENTES, LUIS GERARDO</creator><scope>EVB</scope></search><sort><creationdate>20200915</creationdate><title>PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS</title><author>SANDOVAL RODRIGUEZ, CELSO MIGUEL ; GUTIERREZ FUENTES, LUIS GERARDO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_CA2859852C3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre</language><creationdate>2020</creationdate><topic>CHEMISTRY</topic><topic>FOODS OR FOODSTUFFS</topic><topic>FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BYSUBCLASSES A23B - A23J</topic><topic>HUMAN NECESSITIES</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL</topic><topic>STEROIDS</topic><topic>THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OFNUTRITIVE QUALITIES, PHYSICAL TREATMENT</topic><topic>THEIR TREATMENT, NOT COVERED BY OTHER CLASSES</topic><toplevel>online_resources</toplevel><creatorcontrib>SANDOVAL RODRIGUEZ, CELSO MIGUEL</creatorcontrib><creatorcontrib>GUTIERREZ FUENTES, LUIS GERARDO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>SANDOVAL RODRIGUEZ, CELSO MIGUEL</au><au>GUTIERREZ FUENTES, LUIS GERARDO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS</title><date>2020-09-15</date><risdate>2020</risdate><abstract>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.</abstract><oa>free_for_read</oa></addata></record> |
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| language | eng ; fre |
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| 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 |
| title | PROCESS FOR ALKYNYLATING 16-SUBSTITUTED-17-KETO STEROIDS |
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