MX341561B - Proceso para la produccion de intermediarios de estetrol. - Google Patents
Proceso para la produccion de intermediarios de estetrol.Info
- Publication number
- MX341561B MX341561B MX2013014045A MX2013014045A MX341561B MX 341561 B MX341561 B MX 341561B MX 2013014045 A MX2013014045 A MX 2013014045A MX 2013014045 A MX2013014045 A MX 2013014045A MX 341561 B MX341561 B MX 341561B
- Authority
- MX
- Mexico
- Prior art keywords
- formula
- compound
- reacting
- group
- produce
- Prior art date
Links
- AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title 1
- 229950009589 estetrol Drugs 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 239000003638 chemical reducing agent Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- YJVFFLUZDVXJQI-UHFFFAOYSA-L palladium(ii) acetate Chemical compound [Pd+2].CC([O-])=O.CC([O-])=O YJVFFLUZDVXJQI-UHFFFAOYSA-L 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
- C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0051—Estrane derivatives
- C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
-
- 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
- C07J13/005—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 16 (17)
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161492300P | 2011-06-01 | 2011-06-01 | |
| EP11168561 | 2011-06-01 | ||
| PCT/EP2012/060447 WO2012164096A1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2013014045A MX2013014045A (es) | 2014-08-22 |
| MX341561B true MX341561B (es) | 2016-08-25 |
Family
ID=45003353
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2013014045A MX341561B (es) | 2011-06-01 | 2012-06-01 | Proceso para la produccion de intermediarios de estetrol. |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US11053274B2 (enExample) |
| EP (1) | EP2714710B1 (enExample) |
| JP (2) | JP6425540B2 (enExample) |
| KR (1) | KR101994805B1 (enExample) |
| CN (2) | CN103703014A (enExample) |
| AU (1) | AU2012264602B2 (enExample) |
| BR (1) | BR112013030830B1 (enExample) |
| CA (1) | CA2835981C (enExample) |
| CY (1) | CY1118150T1 (enExample) |
| DK (1) | DK2714710T3 (enExample) |
| EA (1) | EA023991B1 (enExample) |
| ES (1) | ES2579175T3 (enExample) |
| HR (1) | HRP20160692T2 (enExample) |
| HU (1) | HUE029252T2 (enExample) |
| ME (1) | ME02454B (enExample) |
| MX (1) | MX341561B (enExample) |
| PL (1) | PL2714710T3 (enExample) |
| PT (1) | PT2714710T (enExample) |
| RS (1) | RS54880B1 (enExample) |
| SG (1) | SG195118A1 (enExample) |
| SI (1) | SI2714710T1 (enExample) |
| SM (1) | SMT201600206B (enExample) |
| WO (1) | WO2012164096A1 (enExample) |
| ZA (1) | ZA201308446B (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11053274B2 (en) | 2011-06-01 | 2021-07-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
| EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| EP2764008B1 (en) | 2011-10-07 | 2016-08-17 | Estetra S.P.R.L. | Process for the production of estetrol |
| JP6813150B2 (ja) | 2015-06-18 | 2021-01-13 | エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ | エステトロールを含有する口腔内崩壊錠 |
| CN116077454A (zh) | 2015-06-18 | 2023-05-09 | 埃斯特拉有限责任公司 | 含雌四醇组分的口腔分散剂量单位 |
| US11147771B2 (en) | 2015-06-18 | 2021-10-19 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
| CN105837424A (zh) * | 2016-03-31 | 2016-08-10 | 常州大学 | 一种1-氯-3-甲基-3-丁烯-2-酮的合成方法 |
| CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
| JP6935766B2 (ja) | 2018-02-15 | 2021-09-15 | 日本精工株式会社 | スピンドル装置 |
| JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
| TWI801561B (zh) | 2018-04-19 | 2023-05-11 | 比利時商依思特拉私人有限責任公司 | 化合物及其用於緩解絕經相關症狀的用途 |
| IT201900017414A1 (it) | 2019-09-27 | 2021-03-27 | Ind Chimica Srl | Processo per la preparazione di (15α,16α,17β)-estra-1,3,5(10)-triene-3,15,16,17-tetrolo (Estetrolo) ed intermedi di detto processo |
| IT201900021879A1 (it) | 2019-11-22 | 2021-05-22 | Ind Chimica Srl | PROCESSO PER LA PREPARAZIONE DI (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROLO (ESTETROLO) ED INTERMEDI DI DETTO PROCESSO |
| UY38895A (es) | 2019-09-27 | 2021-04-30 | Ind Chimica Srl | PROCESO PARA PREPARAR (15a,16a,17ß)-ESTRA-1,3,5(10)-TRIENO-3,15,16,17-TETROL (ESTETROL) E INTERMEDIOS DE DICHO PROCESO |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
| WO2023021026A1 (en) | 2021-08-17 | 2023-02-23 | Aspen Oss B.V. | A synthetic pathway to estra-1,3,5(10)-triene-3,15a,16a,17b-tetrol |
| GB2626482B (en) | 2021-10-01 | 2025-04-30 | Ind Chimica Srl | Process for preparing (15alpha,16alpha,17beta)-estra-1,3,5-(10)-triene-3,15,16,17-tetrol(estetrol) monohydrate |
| WO2024160373A1 (en) | 2023-02-02 | 2024-08-08 | Industriale Chimica S.R.L. | PROCESS FOR PREPARING (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL (ESTETROL) MONOHYDRATE |
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|---|---|---|---|---|
| DE144266C (enExample) | ||||
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| US3177206A (en) | 1963-03-07 | 1965-04-06 | American Home Prod | Selective bromination of a-ring aromatic 17-ketalized steroids |
| US3433785A (en) | 1966-07-11 | 1969-03-18 | Sterling Drug Inc | 15,16-disubstituted aromatic steroids,intermediates and processes |
| US3673180A (en) | 1970-06-18 | 1972-06-27 | Merck & Co Inc | 19-nor-6,6-ethylene-20-spiroxenes |
| US4792620A (en) | 1983-10-14 | 1988-12-20 | Bp Chemicals Limited | Carbonylation catalysts |
| US4739078A (en) | 1984-02-17 | 1988-04-19 | The Upjohn Company | Use of borohydride-salt lanthanide salt reagents for stereo selective reduction of C-15-keto prostaglandin precursors |
| IE60780B1 (en) | 1987-01-23 | 1994-08-10 | Akzo Nv | New 11-aryl steroid derivatives |
| DE3710728A1 (de) | 1987-03-31 | 1988-10-13 | Schering Ag | Verfahren zur herstellung von 17(alpha)-ethinyl-17ss-hydroxy-18-methyl-4,15-estradien-3-on und die neuen zwischenprodukte fuer dieses verfahren |
| US5073374A (en) | 1988-11-30 | 1991-12-17 | Schering Corporation | Fast dissolving buccal tablet |
| US5340586A (en) | 1991-04-12 | 1994-08-23 | University Of Southern California | Methods and formulations for use in treating oophorectomized women |
| JPH07101977A (ja) | 1993-10-05 | 1995-04-18 | Kureha Chem Ind Co Ltd | ホルモン作用を軽減した新規なエストラジオール誘導体及びその増殖因子阻害剤 |
| WO1997004752A1 (en) | 1995-07-26 | 1997-02-13 | Duramed Pharmaceuticals, Inc. | Pharmaceutical compositions of conjugated estrogens and methods for their use |
| US6117446A (en) | 1999-01-26 | 2000-09-12 | Place; Virgil A. | Drug dosage unit for buccal administration of steroidal active agents |
| TW548277B (en) | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| US20020132801A1 (en) | 2001-01-11 | 2002-09-19 | Schering Aktiengesellschaft | Drospirenone for hormone replacement therapy |
| EP1260225A1 (en) | 2001-05-18 | 2002-11-27 | Pantarhei Bioscience B.V. | A pharmaceutical composition for use in hormone replacement therapy |
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| DK1390042T3 (da) | 2001-05-23 | 2008-03-31 | Pantarhei Bioscience Bv | System for administration af et lægemiddel omfattende tetrahydroxyleret östrogen til anvendelse i hormonal svangerskabsforebyggelse |
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| US6723348B2 (en) | 2001-11-16 | 2004-04-20 | Ethypharm | Orodispersible tablets containing fexofenadine |
| HU227198B1 (en) | 2001-11-27 | 2010-10-28 | Richter Gedeon Nyrt | Pharmaceutical composition for emergency contraception containing levonorgestrel |
| DK1478373T3 (da) | 2002-02-21 | 2007-01-15 | Schering Ag | Farmaceutisk præparat omfattende ét eller flere steroider, én eller flere tetrahydrofolatbestanddele og vitamin B 12 |
| US20050147670A1 (en) | 2002-05-29 | 2005-07-07 | Impax Laboratories Inc. | Oral disintegrating dosage forms |
| CN100352445C (zh) | 2002-06-11 | 2007-12-05 | 潘塔希生物科学股份有限公司 | 一种皮肤护理组合物及其用途 |
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| ES2299730T3 (es) | 2002-07-12 | 2008-06-01 | Pantarhei Bioscience B.V. | Composicion farmaceutica que comprende derivados de estetrol para el uso en la terapia del cancer. |
| CA2503549C (en) | 2002-10-23 | 2012-07-10 | Pantarhei Bioscience B.V. | Pharmaceutical compositions comprising estetrol derivatives for use in cancer therapy |
| ATE469165T1 (de) | 2002-11-08 | 2010-06-15 | Pantarhei Bioscience Bv | Synthese von oestetrol aus von oestron abgeleiteten steroiden |
| ES2274456T3 (es) | 2003-05-22 | 2007-05-16 | Pantarhei Bioscience B.V. | Uso de composiciones que comprenden un componente estrogenico para el tratamiento y la prevencion del dolor musculoesqueletico. |
| ZA200709854B (en) | 2005-05-26 | 2009-03-25 | Solvay Pharm Gmbh | 17ß-HSD1 and STS inhibitors |
| DE112006002611A5 (de) | 2005-07-25 | 2008-07-03 | Technische Universität Dresden | Rna-abhängige rna-polymerase, verfahren und kits zur amplifikation und / oder markierung von rna |
| US20070048369A1 (en) | 2005-08-26 | 2007-03-01 | National Starch And Chemical Investment Holding Corporation | Mucosal delivery tablet |
| CA2636638C (en) | 2006-01-09 | 2014-02-18 | Pantarhei Bioscience B.V. | A method of treating an acute vascular disorder |
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| ATE473746T1 (de) | 2007-01-08 | 2010-07-15 | Pantarhei Bioscience Bv | Verfahren zur behandlung oder prävention von unfruchtbarkeit bei weiblichen säugern und pharmazeutisches kit zur anwendung dieses verfahrens |
| CL2008000095A1 (es) | 2007-01-12 | 2008-05-16 | Wyeth Corp | Composicion de tableta en tableta que comprende una tableta central con estrogenos, un rellenador/diluyente, un rellenador/aglomerante, un componente polimerico y una capa de tableta exterior comprimida con agentes terapeuticos, un rellenador/diluyen |
| ATE537833T1 (de) | 2007-06-21 | 2012-01-15 | Pantarhei Bioscience Bv | Behandlung des mekoniumaspirationssyndroms mit östrogenen |
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| US9603860B2 (en) | 2010-07-28 | 2017-03-28 | Laboratorios Leon Farma Sa | Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same |
| CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
| US11053274B2 (en) | 2011-06-01 | 2021-07-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
| EP2383279A1 (en) * | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
| US10179107B2 (en) | 2011-07-19 | 2019-01-15 | Pantarhei Bioscience B.V. | Tablet containing dehydroepiandrosterone (DHEA) |
| LT2741824T (lt) | 2011-08-11 | 2017-06-26 | Estetra S.P.R.L. | Estetrolio panaudojimas kaip skubaus kontraceptiko |
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| EP2764008B1 (en) | 2011-10-07 | 2016-08-17 | Estetra S.P.R.L. | Process for the production of estetrol |
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| US9808470B2 (en) | 2012-04-19 | 2017-11-07 | Universite De Liege | Estrogenic components for use in the treatment of neurological disorders |
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| CA2924255C (en) | 2013-09-18 | 2022-11-22 | Crystal Pharma, S.A.U. | Process for the preparation of estetrol |
| NZ720906A (en) | 2013-12-12 | 2022-04-29 | Estetra Sprl | Orally disintegrating solid dosage unit containing an estetrol component |
| JP6813150B2 (ja) | 2015-06-18 | 2021-01-13 | エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ | エステトロールを含有する口腔内崩壊錠 |
| US11147771B2 (en) | 2015-06-18 | 2021-10-19 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
| CN116077454A (zh) | 2015-06-18 | 2023-05-09 | 埃斯特拉有限责任公司 | 含雌四醇组分的口腔分散剂量单位 |
-
2012
- 2012-06-01 US US14/122,872 patent/US11053274B2/en active Active
- 2012-06-01 EA EA201301316A patent/EA023991B1/ru unknown
- 2012-06-01 ME MEP-2016-130A patent/ME02454B/me unknown
- 2012-06-01 PL PL12729054T patent/PL2714710T3/pl unknown
- 2012-06-01 KR KR1020137031483A patent/KR101994805B1/ko active Active
- 2012-06-01 HR HRP20160692TT patent/HRP20160692T2/hr unknown
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