BR112018073492A2 - processo e intermediários para a 6,7-alfa epoxidação de esteroide 4,6-dienos - Google Patents
processo e intermediários para a 6,7-alfa epoxidação de esteroide 4,6-dienosInfo
- Publication number
- BR112018073492A2 BR112018073492A2 BR112018073492A BR112018073492A BR112018073492A2 BR 112018073492 A2 BR112018073492 A2 BR 112018073492A2 BR 112018073492 A BR112018073492 A BR 112018073492A BR 112018073492 A BR112018073492 A BR 112018073492A BR 112018073492 A2 BR112018073492 A2 BR 112018073492A2
- Authority
- BR
- Brazil
- Prior art keywords
- intermediates
- epoxidation
- alpha
- diene steroid
- relates
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 238000006735 epoxidation reaction Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000003613 bile acid Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003054 catalyst Substances 0.000 abstract 1
- 239000007800 oxidant agent Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0088—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
- C07J71/0005—Oxygen-containing hetero ring
- C07J71/001—Oxiranes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
- C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
- C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Toxicology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
a presente invenção refere-se a um processo para a preparação de um composto de fórmula geral (ia): (ia) em que r2, y, r4 e r5 são como definidos aqui, em que a expoxidação é conduzida usando um oxidante e metiltrioxorênio como um catalisador (mereo3). a invenção também se refere a certos compostos de per si. os compostos são intermediários na síntese de ácidos biliares sintéticos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1608776.9A GB201608776D0 (en) | 2016-05-18 | 2016-05-18 | Methods and compounds |
PCT/GB2017/051389 WO2017199036A1 (en) | 2016-05-18 | 2017-05-18 | Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112018073492A2 true BR112018073492A2 (pt) | 2019-03-26 |
Family
ID=56320628
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112018073492A BR112018073492A2 (pt) | 2016-05-18 | 2017-05-18 | processo e intermediários para a 6,7-alfa epoxidação de esteroide 4,6-dienos |
Country Status (15)
Country | Link |
---|---|
US (1) | US10766921B2 (pt) |
EP (1) | EP3458467B1 (pt) |
JP (1) | JP7034094B2 (pt) |
KR (1) | KR102489565B1 (pt) |
CN (1) | CN109415404B (pt) |
AU (1) | AU2017265445B2 (pt) |
BR (1) | BR112018073492A2 (pt) |
CA (1) | CA3024283A1 (pt) |
DK (1) | DK3458467T3 (pt) |
EA (1) | EA038224B1 (pt) |
ES (1) | ES2841324T3 (pt) |
GB (1) | GB201608776D0 (pt) |
MX (1) | MX2018014130A (pt) |
PT (1) | PT3458467T (pt) |
WO (1) | WO2017199036A1 (pt) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
CN111560045A (zh) * | 2020-06-23 | 2020-08-21 | 江苏佳尔科药业集团股份有限公司 | 一种以ba为原料合成石胆酸的方法 |
CN114957368A (zh) * | 2021-09-08 | 2022-08-30 | 湖南醇康医药科技有限公司 | 中间体化合物及其制备方法和应用 |
CN114957372B (zh) * | 2021-12-07 | 2023-10-31 | 湖南醇康医药科技有限公司 | 10α-甲基-5,7-二烯甾体化合物和地屈孕酮的制备方法 |
Family Cites Families (36)
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US2624748A (en) | 1950-09-09 | 1953-01-06 | Upjohn Co | Bisnorchola-4, 6-dien-3-one-22-al |
IT1088094B (it) | 1976-10-14 | 1985-06-04 | Hoffmann La Roche | Derivati del pregnano |
US4289872A (en) | 1979-04-06 | 1981-09-15 | Allied Corporation | Macromolecular highly branched homogeneous compound based on lysine units |
US5229490A (en) | 1987-05-06 | 1993-07-20 | The Rockefeller University | Multiple antigen peptide system |
DE3902357A1 (de) | 1989-01-27 | 1990-08-02 | Hoechst Ag | Verwendung von rheniumorganischen verbindungen zur oxidation von c-c-mehrfachbindungen, darauf basierende oxidationsverfahren und neue rheniumorganische verbindungen |
US5166372A (en) | 1992-02-07 | 1992-11-24 | Arco Chemical Technology, L.P. | Epoxidation process |
CA2118130A1 (en) | 1992-04-14 | 1993-10-28 | Jean M. J. Frechet | Dendritic based macromolecules and method of production |
US5643575A (en) | 1993-10-27 | 1997-07-01 | Enzon, Inc. | Non-antigenic branched polymer conjugates |
US5932462A (en) | 1995-01-10 | 1999-08-03 | Shearwater Polymers, Inc. | Multiarmed, monofunctional, polymer for coupling to molecules and surfaces |
US5723636A (en) | 1996-04-12 | 1998-03-03 | National Starch And Chemical Investment Holding Corporation | Methyltrioxorhenium-urea hydrogen peroxide epoxidation of olefins |
US7138390B2 (en) | 2001-03-12 | 2006-11-21 | Intercept Pharmaceuticals | Steroids as agonists for FXR |
US20090062256A1 (en) | 2001-06-01 | 2009-03-05 | Bristol-Myers Squibb Pharma Company | LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION |
CA2466027C (en) | 2001-11-07 | 2013-01-08 | Nektar Therapeutics Al, Corporation | Branched polymers and their conjugates |
ITMI20030352A1 (it) | 2003-02-27 | 2004-08-28 | Chemi Spa | Metodo per la sintesi di metiltriossorenio. |
EP1568706A1 (en) | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
EP1775304A4 (en) | 2004-07-13 | 2010-04-28 | Mitsubishi Chem Corp | PROCESS FOR THE PRODUCTION OF STEROIDS |
ITMI20050912A1 (it) * | 2005-05-19 | 2006-11-20 | Erregierre Spa | Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici |
JP2007210888A (ja) | 2006-01-12 | 2007-08-23 | Mitsubishi Chemicals Corp | ステロイド化合物の製造方法 |
CA2656320C (en) | 2006-06-27 | 2015-04-28 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions |
WO2010014836A2 (en) | 2008-07-30 | 2010-02-04 | Intercept Pharmaceuticals, Inc. | Tgr5 modulators and methods of use thereof |
JP5639073B2 (ja) | 2008-11-19 | 2014-12-10 | インターセプト ファーマシューティカルズ, インコーポレイテッド | Tgr5モジュレーターおよびその使用方法 |
JP2013500986A (ja) | 2009-07-29 | 2013-01-10 | ザ・ユニバーシティ・オブ・シカゴ | 肝臓x受容体アゴニスト |
DK3336097T3 (da) | 2012-06-19 | 2020-09-28 | Intercept Pharmaceuticals Inc | Fremstilling af ikke-krystallinsk obeticholsyre |
NZ745013A (en) | 2012-10-26 | 2019-08-30 | Intercept Pharmaceuticals Inc | Process for preparing bile acid derivatives |
MX2015006710A (es) | 2012-11-28 | 2016-01-15 | Intercept Pharmaceuticals Inc | Tratamiento de las enfermedades pulmonares. |
US20140206657A1 (en) | 2013-01-18 | 2014-07-24 | City Of Hope | Bile acid analog tgr5 agonists |
WO2015183794A1 (en) | 2014-05-27 | 2015-12-03 | City Of Hope | Tgr5 agonist complexes for treating diabetes and cancer |
KR102527821B1 (ko) | 2014-11-19 | 2023-05-02 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드 |
EA033445B1 (ru) | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
CN107108688B (zh) | 2014-11-19 | 2019-10-29 | Nzp英国有限公司 | 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇 |
EP3221331B1 (en) | 2014-11-19 | 2019-09-18 | Nzp Uk Limited | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |
WO2016086115A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof |
CN105348365A (zh) | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一种胆酸衍生物及其制备方法、药物组合物和用途 |
GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
GB201608779D0 (en) * | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
-
2016
- 2016-05-18 GB GBGB1608776.9A patent/GB201608776D0/en not_active Ceased
-
2017
- 2017-05-18 CN CN201780030784.4A patent/CN109415404B/zh active Active
- 2017-05-18 BR BR112018073492A patent/BR112018073492A2/pt unknown
- 2017-05-18 EA EA201892516A patent/EA038224B1/ru unknown
- 2017-05-18 EP EP17725742.5A patent/EP3458467B1/en active Active
- 2017-05-18 JP JP2018560672A patent/JP7034094B2/ja active Active
- 2017-05-18 US US16/302,057 patent/US10766921B2/en active Active
- 2017-05-18 ES ES17725742T patent/ES2841324T3/es active Active
- 2017-05-18 CA CA3024283A patent/CA3024283A1/en active Pending
- 2017-05-18 KR KR1020187035835A patent/KR102489565B1/ko active IP Right Grant
- 2017-05-18 AU AU2017265445A patent/AU2017265445B2/en active Active
- 2017-05-18 DK DK17725742.5T patent/DK3458467T3/da active
- 2017-05-18 MX MX2018014130A patent/MX2018014130A/es unknown
- 2017-05-18 WO PCT/GB2017/051389 patent/WO2017199036A1/en unknown
- 2017-05-18 PT PT177257425T patent/PT3458467T/pt unknown
Also Published As
Publication number | Publication date |
---|---|
AU2017265445B2 (en) | 2020-12-03 |
EP3458467A1 (en) | 2019-03-27 |
KR102489565B1 (ko) | 2023-01-17 |
PT3458467T (pt) | 2021-01-05 |
US20190309012A1 (en) | 2019-10-10 |
AU2017265445A1 (en) | 2018-11-15 |
MX2018014130A (es) | 2019-04-29 |
ES2841324T3 (es) | 2021-07-08 |
WO2017199036A1 (en) | 2017-11-23 |
KR20190007011A (ko) | 2019-01-21 |
EA038224B1 (ru) | 2021-07-27 |
CN109415404A (zh) | 2019-03-01 |
EP3458467B1 (en) | 2020-09-30 |
JP2019516729A (ja) | 2019-06-20 |
GB201608776D0 (en) | 2016-06-29 |
EA201892516A1 (ru) | 2019-05-31 |
CA3024283A1 (en) | 2017-11-23 |
DK3458467T3 (da) | 2020-12-14 |
JP7034094B2 (ja) | 2022-03-11 |
US10766921B2 (en) | 2020-09-08 |
CN109415404B (zh) | 2022-08-26 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
B15K | Others concerning applications: alteration of classification |
Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07J 9/00 , C07J 71/00 Ipc: C07J 9/00 (2006.01), C07J 71/00 (2006.01), A61P 1/ |
|
B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |