Methods for the preparation of drospirenone and intermediates thereof
The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wher...
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| creator | GAMBARIN LUCA ANDRIOLO ERIKA MONTORSI MAURO SCALAPRICE ROMEO MERLO MASSIMO ORRU′ GIANMAURO MARIANI EDOARDO |
| description | The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too. |
| format | Patent |
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New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; STEROIDS</subject><creationdate>2014</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=20140923&DB=EPODOC&CC=US&NR=8841283B2$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,778,883,25551,76302</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20140923&DB=EPODOC&CC=US&NR=8841283B2$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>GAMBARIN LUCA</creatorcontrib><creatorcontrib>ANDRIOLO ERIKA</creatorcontrib><creatorcontrib>MONTORSI MAURO</creatorcontrib><creatorcontrib>SCALAPRICE ROMEO</creatorcontrib><creatorcontrib>MERLO MASSIMO</creatorcontrib><creatorcontrib>ORRU′ GIANMAURO</creatorcontrib><creatorcontrib>MARIANI EDOARDO</creatorcontrib><title>Methods for the preparation of drospirenone and intermediates thereof</title><description>The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</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>STEROIDS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2014</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNyzEOwjAMRuEsDAi4gy_AQMuQGVTUpRMwVxb5o0aiduT4_kJIHIDpLd_bhmGCL5oaZTXyBVQNlY29qJBmSqatFoOogFgSFXHYilTY0b6HQfM-bDK_Gw6_7gLdhsd1PKLqjFb5BYHPz3uM51MX-0vX_0E-xqYzfg</recordid><startdate>20140923</startdate><enddate>20140923</enddate><creator>GAMBARIN LUCA</creator><creator>ANDRIOLO ERIKA</creator><creator>MONTORSI MAURO</creator><creator>SCALAPRICE ROMEO</creator><creator>MERLO MASSIMO</creator><creator>ORRU′ GIANMAURO</creator><creator>MARIANI EDOARDO</creator><scope>EVB</scope></search><sort><creationdate>20140923</creationdate><title>Methods for the preparation of drospirenone and intermediates thereof</title><author>GAMBARIN LUCA ; ANDRIOLO ERIKA ; MONTORSI MAURO ; SCALAPRICE ROMEO ; MERLO MASSIMO ; ORRU′ GIANMAURO ; MARIANI EDOARDO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_US8841283B23</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2014</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</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>STEROIDS</topic><toplevel>online_resources</toplevel><creatorcontrib>GAMBARIN LUCA</creatorcontrib><creatorcontrib>ANDRIOLO ERIKA</creatorcontrib><creatorcontrib>MONTORSI MAURO</creatorcontrib><creatorcontrib>SCALAPRICE ROMEO</creatorcontrib><creatorcontrib>MERLO MASSIMO</creatorcontrib><creatorcontrib>ORRU′ GIANMAURO</creatorcontrib><creatorcontrib>MARIANI EDOARDO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>GAMBARIN LUCA</au><au>ANDRIOLO ERIKA</au><au>MONTORSI MAURO</au><au>SCALAPRICE ROMEO</au><au>MERLO MASSIMO</au><au>ORRU′ GIANMAURO</au><au>MARIANI EDOARDO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>Methods for the preparation of drospirenone and intermediates thereof</title><date>2014-09-23</date><risdate>2014</risdate><abstract>The invention relates to a process for the preparation of Drospirenone in high yields and purity starting from a compound of formula 2 wherein R is a hydroxyl protective group as defined in the claims, through a sequence of oxidation, deprotection, lactonization and water elimination steps, and wherein the steps of oxidation and lactonization are performed with 1,3,5-trichloro1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (trichloroisocyanuric acid, TCCA) or 1,3-dichloro-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione (dichloroisocyanuric acid, DCCA) or an alkaline metal salt thereof such as the sodium salt dihydrate (DCCA sodium salt) or 1-hydroxy-1,2-benziodoxol-3(1H)-one 1-oxide (IBX). New synthetic intermediates useful for the synthesis of Drospirenone are disclosed, too.</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES STEROIDS |
| title | Methods for the preparation of drospirenone and intermediates thereof |
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