NO20070747L - Metode for fremstilling av 2-substituerte derivater av estron og estradiol - Google Patents
Metode for fremstilling av 2-substituerte derivater av estron og estradiolInfo
- Publication number
- NO20070747L NO20070747L NO20070747A NO20070747A NO20070747L NO 20070747 L NO20070747 L NO 20070747L NO 20070747 A NO20070747 A NO 20070747A NO 20070747 A NO20070747 A NO 20070747A NO 20070747 L NO20070747 L NO 20070747L
- Authority
- NO
- Norway
- Prior art keywords
- compound
- general formula
- preparing
- estrone
- estradiol
- Prior art date
Links
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical class OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 title abstract 2
- 229960005309 estradiol Drugs 0.000 title abstract 2
- 229930182833 estradiol Chemical class 0.000 title abstract 2
- 150000002167 estrones Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 9
- 239000000543 intermediate Substances 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- DNXHEGUUPJUMQT-CBZIJGRNSA-N Estrone Chemical class OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 DNXHEGUUPJUMQT-CBZIJGRNSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 230000001076 estrogenic effect Effects 0.000 abstract 1
- 229960003399 estrone Drugs 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- 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
- C07J75/00—Processes for the preparation of steroids in general
- C07J75/005—Preparation of steroids by cyclization of non-steroid compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Steroid Compounds (AREA)
- Pyrane Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
Oppfinnelsen tilveiebringer en fremgangsmåte for fremstilling av 2-substituerte derivater av østron og østradiol, som omfatter i) fremstilling av en forbindelse med den generelle formel (II) ved omsetning av en forbindelse med den generelle formel (I) i ett eller flere trinn, til en forbindelse med den generelle formel II hvor R1 er en C1-C10 alkyl-, alkenyl- eller arylgruppe; -Cl, -Br, -I, -F; -CN; -OH; eller en -OR2-, -O(CO)R2- eller -R2-OH-gruppe, hvor R2 er en alkyl- eller alkylengruppe som har 1-6 C atomer; og bindingen mellom atom 9 og 10 er en enkelt- eller dobbeltbinding; ii) aromatisering av forbindelsen med den generelle formel II til en forbindelse med den generelle formel III hvor R1 og R2 har de ovenfor definerte betydninger; og iii) eventuelt reduksjon av forbindelsen med den generelle formel III til en forbindelse med den generelle formel IV hvor R1 og R2 har de ovenfor definerte betydninger. Videre tilveiebringer oppfinnelsen flere nye forbindelser som kan være mellomprodukter i fremgangsmåten ovenfor, og fremgangsmåter for fremstilling av disse nye forbindelsene. Oppfinnelsen tilveiebringer også 2-alkoksy-østron, 2-alkoksy-østradiol eller blandinger derav, som er hovedsakelig fri for andre østrogene mellomprodukter.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04103742 | 2004-08-04 | ||
| PCT/EP2005/053732 WO2006013196A1 (en) | 2004-08-04 | 2005-08-01 | Process for the preparation 2-substituted-derivatives of estrone and estradiol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NO20070747L true NO20070747L (no) | 2007-04-23 |
Family
ID=34929415
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20070747A NO20070747L (no) | 2004-08-04 | 2007-02-08 | Metode for fremstilling av 2-substituerte derivater av estron og estradiol |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US7910756B2 (no) |
| EP (1) | EP1776378B1 (no) |
| JP (1) | JP5075626B2 (no) |
| KR (1) | KR20070040386A (no) |
| CN (1) | CN1993376A (no) |
| AR (1) | AR050195A1 (no) |
| AT (1) | ATE447580T1 (no) |
| AU (1) | AU2005268768B2 (no) |
| BR (1) | BRPI0514096A (no) |
| CA (1) | CA2573133C (no) |
| DE (1) | DE602005017500D1 (no) |
| EC (1) | ECSP077228A (no) |
| ES (1) | ES2334244T3 (no) |
| IL (1) | IL180381A0 (no) |
| MX (1) | MX2007001340A (no) |
| NO (1) | NO20070747L (no) |
| RU (1) | RU2007107914A (no) |
| TW (1) | TW200611909A (no) |
| WO (1) | WO2006013196A1 (no) |
| ZA (1) | ZA200700483B (no) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ2008275A3 (cs) | 2008-05-05 | 2009-05-06 | Prírodovedecká Fakulta Uk | Ligandy estrogenových receptoru alfa a beta, zpusob jejich prípravy a farmaceutické prostredky, které je obsahují |
| WO2012020417A1 (en) | 2010-08-10 | 2012-02-16 | Reliance Life Sciences Pvt. Ltd. | Process for the preparation of estradiol and its derivatives |
| EP2742352B1 (en) * | 2011-08-12 | 2018-02-28 | Siemens Healthcare Diagnostics Inc. | Detection of sex steroids |
| CN104497088B (zh) * | 2014-12-30 | 2016-08-24 | 湖南新合新生物医药有限公司 | 19-去甲-4-雄甾烯-3,17-二酮的制备方法 |
| CN104592339A (zh) * | 2014-12-30 | 2015-05-06 | 湖南新合新生物医药有限公司 | 雌甾-4,9-二烯-3,17-二酮的制备方法 |
| ITUB20155260A1 (it) * | 2015-10-30 | 2017-04-30 | Ind Chimica Srl | PROCESSO PER LA PREPARAZIONE DI 17?-idrossi-des-A-androst-9,10-en-5-one |
| CN108003210A (zh) * | 2018-01-24 | 2018-05-08 | 四川理工学院 | 一种雌甾-4,9-二烯-3,17-二酮的制备方法 |
| CN108997463B (zh) * | 2018-08-09 | 2021-05-14 | 四川理工学院 | 一种雌甾-4，9-二烯-3，17-二酮制备方法 |
| CN112409434B (zh) * | 2020-11-27 | 2021-10-26 | 厦门欧瑞捷生物科技有限公司 | 一种去氢孕酮的合成方法 |
| CN113861158B (zh) * | 2021-11-22 | 2023-02-10 | 湖南新合新生物医药有限公司 | 一种合成甲基双烯双酮关键中间体的方法 |
| CN114853802B (zh) * | 2022-03-22 | 2023-11-28 | 河北康泰药业有限公司 | 一种谷内酯衍生物及其制备方法、药物组合物和应用 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2997488A (en) * | 1959-06-20 | 1961-08-22 | Organon | 2-methyl-19-nor-steroids |
| FR1468608A (fr) * | 1960-08-04 | 1967-02-10 | Upjohn Co | 2-alpha-fluoro stéroïdes de la série de la 19-norandrostène et leur procédé d'obtention |
| FR1368721A (fr) | 1961-04-14 | 1964-08-07 | Roussel Uclaf | Dérivés de la 19-nor testostérone et procédé de préparation |
| BE616293A (fr) | 1961-04-14 | 1962-10-11 | Roussel Uclaf | Dérivés de la 19-nor testostérone et procédé de préparation |
| US3519714A (en) | 1966-03-15 | 1970-07-07 | Herchel Smith | Synthesis of gona-1,3,5(10)-trienes |
| US4400524A (en) | 1981-07-28 | 1983-08-23 | The Upjohn Company | Grignard reagents prepared from 5-halopentan-2-one propylene ketals |
| DE3208432A1 (de) | 1982-03-09 | 1983-09-15 | The Upjohn Co., 49001 Kalamazoo, Mich. | Verfahren zur herstellung von 19-norandrostendion, zwischenprodukt des 19-norandrostendions und verfahren zu seiner herstellung |
| US5504074A (en) | 1993-08-06 | 1996-04-02 | Children's Medical Center Corporation | Estrogenic compounds as anti-angiogenic agents |
| US5521168A (en) | 1994-10-13 | 1996-05-28 | Alcon Laboratories, Inc. | Estrogen metabolites for lowering intraocular pressure |
| US5998639A (en) | 1995-11-06 | 1999-12-07 | Akzo Nobel, N.V. | Sulfatation of estrogen mixtures |
| IL119649A (en) | 1995-11-30 | 2002-03-10 | Akzo Nobel Nv | Preparation of Cyclic Kills of History - 3 keto- (5) 10, (-9) 11 steroidadians |
| US6051726A (en) | 1997-03-13 | 2000-04-18 | Pharm-Eco Laboratories, Inc. | Synthesis of 2-alkoxyestradiols |
| US7087592B1 (en) | 1999-08-23 | 2006-08-08 | Entre Med, Inc. | Compositions comprising purified 2-methoxyestradiol and methods of producing same |
| AU7572600A (en) | 1999-08-23 | 2001-03-19 | Entremed, Inc | Methods of obtaining 2-methoxyestradiol of high purity |
| EP1343803A2 (en) | 2000-11-27 | 2003-09-17 | EntreMed, Inc. | 2-substituted estrogens as antiangiogenic agents |
-
2005
- 2005-07-14 TW TW094123942A patent/TW200611909A/zh unknown
- 2005-08-01 CA CA2573133A patent/CA2573133C/en not_active Expired - Fee Related
- 2005-08-01 AT AT05767940T patent/ATE447580T1/de not_active IP Right Cessation
- 2005-08-01 JP JP2007524335A patent/JP5075626B2/ja not_active Expired - Fee Related
- 2005-08-01 CN CNA2005800261640A patent/CN1993376A/zh active Pending
- 2005-08-01 MX MX2007001340A patent/MX2007001340A/es active IP Right Grant
- 2005-08-01 KR KR1020077002976A patent/KR20070040386A/ko not_active Ceased
- 2005-08-01 US US11/659,147 patent/US7910756B2/en not_active Expired - Fee Related
- 2005-08-01 AU AU2005268768A patent/AU2005268768B2/en not_active Ceased
- 2005-08-01 RU RU2007107914/04A patent/RU2007107914A/ru not_active Application Discontinuation
- 2005-08-01 WO PCT/EP2005/053732 patent/WO2006013196A1/en not_active Ceased
- 2005-08-01 EP EP05767940A patent/EP1776378B1/en not_active Expired - Lifetime
- 2005-08-01 BR BRPI0514096-0A patent/BRPI0514096A/pt not_active IP Right Cessation
- 2005-08-01 ES ES05767940T patent/ES2334244T3/es not_active Expired - Lifetime
- 2005-08-01 DE DE602005017500T patent/DE602005017500D1/de not_active Expired - Lifetime
- 2005-08-04 AR ARP050103233A patent/AR050195A1/es unknown
-
2006
- 2006-12-27 IL IL180381A patent/IL180381A0/en unknown
-
2007
- 2007-01-16 ZA ZA200700483A patent/ZA200700483B/xx unknown
- 2007-02-05 EC EC2007007228A patent/ECSP077228A/es unknown
- 2007-02-08 NO NO20070747A patent/NO20070747L/no not_active Application Discontinuation
-
2011
- 2011-02-22 US US13/031,975 patent/US20110152544A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP1776378B1 (en) | 2009-11-04 |
| US20110152544A1 (en) | 2011-06-23 |
| MX2007001340A (es) | 2007-03-27 |
| AU2005268768A1 (en) | 2006-02-09 |
| WO2006013196A1 (en) | 2006-02-09 |
| JP2008509109A (ja) | 2008-03-27 |
| ES2334244T3 (es) | 2010-03-08 |
| KR20070040386A (ko) | 2007-04-16 |
| CN1993376A (zh) | 2007-07-04 |
| AR050195A1 (es) | 2006-10-04 |
| US7910756B2 (en) | 2011-03-22 |
| IL180381A0 (en) | 2007-06-03 |
| ECSP077228A (es) | 2007-03-29 |
| RU2007107914A (ru) | 2008-09-10 |
| EP1776378A1 (en) | 2007-04-25 |
| AU2005268768B2 (en) | 2011-10-13 |
| CA2573133A1 (en) | 2006-02-09 |
| TW200611909A (en) | 2006-04-16 |
| ZA200700483B (en) | 2008-09-25 |
| US20090012319A1 (en) | 2009-01-08 |
| CA2573133C (en) | 2012-07-10 |
| BRPI0514096A (pt) | 2008-05-27 |
| DE602005017500D1 (de) | 2009-12-17 |
| ATE447580T1 (de) | 2009-11-15 |
| JP5075626B2 (ja) | 2012-11-21 |
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| FC2A | Withdrawal, rejection or dismissal of laid open patent application |