METHOD FOR PREPARING beta-SUBSTITUTED 4-AZAANDROSTENE
FIELD: chemical industry. SUBSTANCE: present invention describes beta-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C1-3 alkyl; R is carboxamide group, mono- or disubstituted by C1-8 alkyl group(s); or free carboxy group etherified by C1-15 alcohol; and is si...
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| creator | BALOG GABOR KHORVAT JUDIT TUBA ZOLTAN SELESH JANOSH KOLLAR LASLO |
| description | FIELD: chemical industry. SUBSTANCE: present invention describes beta-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C1-3 alkyl; R is carboxamide group, mono- or disubstituted by C1-8 alkyl group(s); or free carboxy group etherified by C1-15 alcohol; and is single or double bond. Present invention also describes preparation of salts of said compounds. Method comprises reacting 17-halogen-4- azaandrostene of general formula (II): wherein R and are defined as above, and X is chlorine, bromine or iodine, with primary or secondary alkyl amine or with C1-5 alcohol in dimethylformamide or dimethylsulfoxide in the presence of palladium (II) salt and phosphines or palladium (II)-base complex as tertiary amine under carbon monoxide atmosphere at 35-80 C and, if desired, converting the resulting compound of general formula I into the other compound of general formula I by hydrogenation, hydrolysis or salt-forming reactions. EFFECT: more efficient preparation method. |
| format | Patent |
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SUBSTANCE: present invention describes beta-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C1-3 alkyl; R is carboxamide group, mono- or disubstituted by C1-8 alkyl group(s); or free carboxy group etherified by C1-15 alcohol; and is single or double bond. Present invention also describes preparation of salts of said compounds. Method comprises reacting 17-halogen-4- azaandrostene of general formula (II): wherein R and are defined as above, and X is chlorine, bromine or iodine, with primary or secondary alkyl amine or with C1-5 alcohol in dimethylformamide or dimethylsulfoxide in the presence of palladium (II) salt and phosphines or palladium (II)-base complex as tertiary amine under carbon monoxide atmosphere at 35-80 C and, if desired, converting the resulting compound of general formula I into the other compound of general formula I by hydrogenation, hydrolysis or salt-forming reactions. EFFECT: more efficient preparation method.</description><edition>6</edition><language>eng</language><subject>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</subject><creationdate>1998</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=19980427&DB=EPODOC&CC=RU&NR=2109746C1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19980427&DB=EPODOC&CC=RU&NR=2109746C1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>BALOG GABOR</creatorcontrib><creatorcontrib>KHORVAT JUDIT</creatorcontrib><creatorcontrib>TUBA ZOLTAN</creatorcontrib><creatorcontrib>SELESH JANOSH</creatorcontrib><creatorcontrib>KOLLAR LASLO</creatorcontrib><title>METHOD FOR PREPARING beta-SUBSTITUTED 4-AZAANDROSTENE</title><description>FIELD: chemical industry. SUBSTANCE: present invention describes beta-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C1-3 alkyl; R is carboxamide group, mono- or disubstituted by C1-8 alkyl group(s); or free carboxy group etherified by C1-15 alcohol; and is single or double bond. Present invention also describes preparation of salts of said compounds. Method comprises reacting 17-halogen-4- azaandrostene of general formula (II): wherein R and are defined as above, and X is chlorine, bromine or iodine, with primary or secondary alkyl amine or with C1-5 alcohol in dimethylformamide or dimethylsulfoxide in the presence of palladium (II) salt and phosphines or palladium (II)-base complex as tertiary amine under carbon monoxide atmosphere at 35-80 C and, if desired, converting the resulting compound of general formula I into the other compound of general formula I by hydrogenation, hydrolysis or salt-forming reactions. EFFECT: more efficient preparation method.</description><subject>CHEMISTRY</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><subject>STEROIDS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1998</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZDD1dQ3x8HdRcPMPUggIcg1wDPL0c1dISi1J1A0OdQoO8QwJDXF1UTDRdYxydPRzCfIPDnH1c-VhYE1LzClO5YXS3AwKbq4hzh66qQX58anFBYnJqXmpJfFBoUaGBpbmJmbOhsZEKAEA7OIoDw</recordid><startdate>19980427</startdate><enddate>19980427</enddate><creator>BALOG GABOR</creator><creator>KHORVAT JUDIT</creator><creator>TUBA ZOLTAN</creator><creator>SELESH JANOSH</creator><creator>KOLLAR LASLO</creator><scope>EVB</scope></search><sort><creationdate>19980427</creationdate><title>METHOD FOR PREPARING beta-SUBSTITUTED 4-AZAANDROSTENE</title><author>BALOG GABOR ; KHORVAT JUDIT ; TUBA ZOLTAN ; SELESH JANOSH ; KOLLAR LASLO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_RU2109746C13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>1998</creationdate><topic>CHEMISTRY</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><topic>STEROIDS</topic><toplevel>online_resources</toplevel><creatorcontrib>BALOG GABOR</creatorcontrib><creatorcontrib>KHORVAT JUDIT</creatorcontrib><creatorcontrib>TUBA ZOLTAN</creatorcontrib><creatorcontrib>SELESH JANOSH</creatorcontrib><creatorcontrib>KOLLAR LASLO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>BALOG GABOR</au><au>KHORVAT JUDIT</au><au>TUBA ZOLTAN</au><au>SELESH JANOSH</au><au>KOLLAR LASLO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>METHOD FOR PREPARING beta-SUBSTITUTED 4-AZAANDROSTENE</title><date>1998-04-27</date><risdate>1998</risdate><abstract>FIELD: chemical industry. SUBSTANCE: present invention describes beta-substituted 4-azaandrostene derivatives of general formula I: wherein R is hydrogen or C1-3 alkyl; R is carboxamide group, mono- or disubstituted by C1-8 alkyl group(s); or free carboxy group etherified by C1-15 alcohol; and is single or double bond. Present invention also describes preparation of salts of said compounds. Method comprises reacting 17-halogen-4- azaandrostene of general formula (II): wherein R and are defined as above, and X is chlorine, bromine or iodine, with primary or secondary alkyl amine or with C1-5 alcohol in dimethylformamide or dimethylsulfoxide in the presence of palladium (II) salt and phosphines or palladium (II)-base complex as tertiary amine under carbon monoxide atmosphere at 35-80 C and, if desired, converting the resulting compound of general formula I into the other compound of general formula I by hydrogenation, hydrolysis or salt-forming reactions. EFFECT: more efficient preparation method.</abstract><edition>6</edition><oa>free_for_read</oa></addata></record> |
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| 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 |
| title | METHOD FOR PREPARING beta-SUBSTITUTED 4-AZAANDROSTENE |
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