NO20031701L - Fremgangsmåte og mellomprodukter i fremstilling av 7- substituerte antiöstrogener - Google Patents
Fremgangsmåte og mellomprodukter i fremstilling av 7- substituerte antiöstrogenerInfo
- Publication number
- NO20031701L NO20031701L NO20031701A NO20031701A NO20031701L NO 20031701 L NO20031701 L NO 20031701L NO 20031701 A NO20031701 A NO 20031701A NO 20031701 A NO20031701 A NO 20031701A NO 20031701 L NO20031701 L NO 20031701L
- Authority
- NO
- Norway
- Prior art keywords
- group
- preparation
- intermediates
- formula
- antiestrogens
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- 229940046836 anti-estrogen Drugs 0.000 title 1
- 230000001833 anti-estrogenic effect Effects 0.000 title 1
- 239000000328 estrogen antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000002243 precursor Substances 0.000 abstract 2
- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229960002258 fulvestrant Drugs 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000962 organic group Chemical group 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
-
- 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)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Fremgangsmåte for fremstilling av en mellomprodukt-forbindelse med formel (II): hvor X er som definert i beskrivelsen, Rer halogenalkyl, alkyl, alkenyl, cykloalkyl, karboksyalkyl, alkoksykarbonylalkyl, aryl eller arylalkyl; R, R, Rog Rer organiske grupper som definert i beskrivelsen, hvilken fremgangsmåte omfatter aromatisering av en forbindelse med formel (EI): hvor R1, R2, R3, n, X og R5 er som definert i forbindelse med formel (II) og R4 er en gruppe Reller en forløpergruppe derav, og deretter, hvis nødvendig eller ønsket, utførelse av ett eller flere av de følgende trinn: (i) fjerning av hvilke som helst hydroksybeskyttelsesgrupper R; (ii) omdannelse av en forløper gruppe R4 til en gruppe R, eller hvor Rer en gruppe R, omdannelse av den til en annen slik gruppe. Forbindelser som blir oppnådd er anvendelige mellomprodukter for eksempel ved fremstilling av fulvestrant. Nye mellomprodukter er også krevet.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0025221.3A GB0025221D0 (en) | 2000-10-14 | 2000-10-14 | New process |
| PCT/GB2001/004485 WO2002032922A1 (en) | 2000-10-14 | 2001-10-09 | Process and intermediates for the production of 7-substituted antiestrogens |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| NO20031701D0 NO20031701D0 (no) | 2003-04-11 |
| NO20031701L true NO20031701L (no) | 2003-05-23 |
| NO326020B1 NO326020B1 (no) | 2008-09-01 |
Family
ID=9901292
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20031701A NO326020B1 (no) | 2000-10-14 | 2003-04-11 | Fremgangsmate for fremstilling av 7-substituerte antiostrogener |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US7947667B2 (no) |
| EP (2) | EP1328538B1 (no) |
| JP (2) | JP4363846B2 (no) |
| KR (2) | KR100864266B1 (no) |
| CN (1) | CN1255425C (no) |
| AR (2) | AR034561A1 (no) |
| AT (1) | ATE403667T1 (no) |
| AU (3) | AU9213201A (no) |
| BR (1) | BR0114649A (no) |
| CA (1) | CA2425572C (no) |
| CY (1) | CY1108398T1 (no) |
| DE (1) | DE60135240D1 (no) |
| DK (1) | DK1328538T3 (no) |
| EG (1) | EG23373A (no) |
| ES (2) | ES2309094T3 (no) |
| GB (1) | GB0025221D0 (no) |
| IL (2) | IL155172A0 (no) |
| MX (1) | MXPA03003302A (no) |
| MY (2) | MY145819A (no) |
| NO (1) | NO326020B1 (no) |
| NZ (1) | NZ525096A (no) |
| PT (1) | PT1328538E (no) |
| SA (1) | SA01220570B1 (no) |
| SI (1) | SI1328538T1 (no) |
| WO (1) | WO2002032922A1 (no) |
| ZA (1) | ZA200302526B (no) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0025221D0 (en) | 2000-10-14 | 2000-11-29 | Astrazeneca Ab | New process |
| GB0123961D0 (en) | 2001-10-05 | 2001-11-28 | Astrazeneca Ab | Process and intermediates |
| JP2007506805A (ja) * | 2004-07-27 | 2007-03-22 | シコール インコーポレイティド | 7α−アルキル化された19−ノルステロイドの調製方法 |
| US20100174101A1 (en) * | 2007-09-24 | 2010-07-08 | Xi'an Liband Pharmaceutical Co., Ltd. | Process for the manufacture of 7-alpha-[9-(4,4,5,5,5-penta fluoropentylsulphinyl) nonyl]estra-1,3,5-(10)- triene-3,17-beta-diol |
| EP2070942A1 (de) | 2007-12-13 | 2009-06-17 | Bayer Schering Pharma Aktiengesellschaft | Verfahren zur Aromatisierung von 19-Nor-androst-4-en-3-onen zu Estra-1,3,5(10)-trienen |
| CN101525364B (zh) * | 2008-03-07 | 2012-12-12 | 杭州九源基因工程有限公司 | 一种氟维司群的晶型及其制备方法 |
| US8063249B1 (en) | 2008-04-25 | 2011-11-22 | Olema Pharmaceuticals, Inc. | Substituted triphenyl butenes |
| CN102391341B (zh) * | 2011-08-09 | 2013-05-22 | 福建省微生物研究所 | 制备6,7-脱氢-17β-烃酰氧基诺龙的方法 |
| CN102600064A (zh) * | 2012-03-31 | 2012-07-25 | 西安力邦制药有限公司 | 氟维司群或其衍生物缓释制剂及其制备方法 |
| EP2909224B1 (en) | 2012-10-22 | 2020-03-18 | Intas Pharmaceuticals Limited | An improved process for the preparation of fulvestrant |
| CN103788164A (zh) * | 2012-10-31 | 2014-05-14 | 正大天晴药业集团股份有限公司 | 一种氟维司群的制备方法 |
| CN103965280B (zh) * | 2014-05-21 | 2016-04-20 | 天津孚音生物科技发展有限公司 | 一种氟维司群中间体的制备方法 |
| WO2015181116A1 (en) | 2014-05-26 | 2015-12-03 | Crystal Pharma, S.A.U. | Process and intermediades for the preparation of 7-alkylated steroids |
| CN104387435B (zh) * | 2014-12-10 | 2017-05-10 | 天津孚音生物科技发展有限公司 | 一种化合物及其制备方法与应用 |
| KR101640747B1 (ko) | 2015-05-20 | 2016-07-19 | 이금운 | 확장 가능형 끼움식 엘이디 조명 등기구 |
| CN107488205A (zh) * | 2016-06-13 | 2017-12-19 | 重庆圣华曦药业股份有限公司 | 一种氟维司群有关物质的制备方法及其在制剂中的检测方法 |
| CN110818764A (zh) * | 2018-08-07 | 2020-02-21 | 重庆圣华曦药业股份有限公司 | 一种应用加料监测系统制备氟维斯群中间体的方法 |
| CN111018936B (zh) * | 2019-11-12 | 2021-10-29 | 广州曼翔医药有限公司 | 一种氟维司群有关物质e的合成方法 |
| CN116041412A (zh) * | 2023-01-13 | 2023-05-02 | 香港中文大学(深圳) | 氟维司群衍生物及其制备方法、应用和治疗乳腺癌的药物 |
| CN116284195B (zh) * | 2023-02-08 | 2025-07-01 | 湖南欧亚药业有限公司 | 一种氟维司群的制备方法 |
| CN116535454A (zh) * | 2023-04-28 | 2023-08-04 | 香港中文大学(深圳) | 氟维司群类化合物及其制备方法和应用 |
| WO2025195993A1 (en) | 2024-03-18 | 2025-09-25 | Minakem | Process for the preparation of fulvestrant |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NL7305171A (no) * | 1973-04-13 | 1974-10-15 | ||
| GB8327256D0 (en) * | 1983-10-12 | 1983-11-16 | Ici Plc | Steroid derivatives |
| US5595985A (en) * | 1989-03-10 | 1997-01-21 | Endorecherche Inc. | Combination therapy for prophylaxis and/or treatment of benign prostatic hyperplasia |
| DE4132182A1 (de) | 1991-09-24 | 1993-03-25 | Schering Ag | 11(beta)-substituierte 14, 17-ethanoestratriene, verfahren zur herstellung dieser verbindungen, sowie ihre verwendung zur herstellung von arzneimitteln |
| US5211831A (en) * | 1991-11-27 | 1993-05-18 | Mcgean-Rohco, Inc. | Process for extending the life of a displacement plating bath |
| DE19622457A1 (de) * | 1996-05-24 | 1997-11-27 | Schering Ag | 7alpha-(5-Methylaminopentyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha-(5-Methylaminopentyl)-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| US5952319A (en) * | 1997-11-26 | 1999-09-14 | Research Triangle Institute | Androgenic steroid compounds and a method of making and using the same |
| ATE334682T1 (de) * | 2000-03-31 | 2006-08-15 | Us Gov Health & Human Serv | Verfahren zur herstellung von den trans-4-n- butylcyclohexanoicsaüre- und undecanoicsaüreestern von (7-alpha,11-beta)- dimethyl-17 beta -hydroxy-4-estren-3-one und deren medizynische anwendung |
| GB0025221D0 (en) | 2000-10-14 | 2000-11-29 | Astrazeneca Ab | New process |
| GB0123961D0 (en) * | 2001-10-05 | 2001-11-28 | Astrazeneca Ab | Process and intermediates |
-
2000
- 2000-10-14 GB GBGB0025221.3A patent/GB0025221D0/en not_active Ceased
-
2001
- 2001-10-09 KR KR1020037005110A patent/KR100864266B1/ko not_active Expired - Lifetime
- 2001-10-09 DK DK01972358T patent/DK1328538T3/da active
- 2001-10-09 EP EP01972358A patent/EP1328538B1/en not_active Expired - Lifetime
- 2001-10-09 IL IL15517201A patent/IL155172A0/xx unknown
- 2001-10-09 BR BR0114649-1A patent/BR0114649A/pt not_active Application Discontinuation
- 2001-10-09 JP JP2002536303A patent/JP4363846B2/ja not_active Expired - Lifetime
- 2001-10-09 US US10/398,924 patent/US7947667B2/en not_active Expired - Fee Related
- 2001-10-09 SI SI200130863T patent/SI1328538T1/sl unknown
- 2001-10-09 AU AU9213201A patent/AU9213201A/xx active Pending
- 2001-10-09 AT AT01972358T patent/ATE403667T1/de active
- 2001-10-09 ES ES01972358T patent/ES2309094T3/es not_active Expired - Lifetime
- 2001-10-09 DE DE60135240T patent/DE60135240D1/de not_active Expired - Lifetime
- 2001-10-09 CA CA002425572A patent/CA2425572C/en not_active Expired - Lifetime
- 2001-10-09 PT PT01972358T patent/PT1328538E/pt unknown
- 2001-10-09 MX MXPA03003302A patent/MXPA03003302A/es active IP Right Grant
- 2001-10-09 NZ NZ525096A patent/NZ525096A/en not_active IP Right Cessation
- 2001-10-09 AU AU2001292132A patent/AU2001292132B2/en not_active Expired
- 2001-10-09 CN CNB018202705A patent/CN1255425C/zh not_active Expired - Lifetime
- 2001-10-09 ES ES08150796.4T patent/ES2581379T3/es not_active Expired - Lifetime
- 2001-10-09 WO PCT/GB2001/004485 patent/WO2002032922A1/en not_active Ceased
- 2001-10-09 KR KR1020087013092A patent/KR20080056029A/ko not_active Ceased
- 2001-10-09 EP EP08150796.4A patent/EP1918295B1/en not_active Expired - Lifetime
- 2001-10-10 EG EG20011065A patent/EG23373A/xx active
- 2001-10-12 MY MYPI20014756A patent/MY145819A/en unknown
- 2001-10-12 MY MYPI2010001633A patent/MY149146A/en unknown
- 2001-10-12 AR ARP010104814A patent/AR034561A1/es active IP Right Grant
- 2001-12-04 SA SA01220570A patent/SA01220570B1/ar unknown
-
2003
- 2003-03-31 IL IL155172A patent/IL155172A/en active IP Right Grant
- 2003-03-31 ZA ZA200302526A patent/ZA200302526B/en unknown
- 2003-04-11 NO NO20031701A patent/NO326020B1/no not_active IP Right Cessation
-
2007
- 2007-04-19 AU AU2007201740A patent/AU2007201740B2/en not_active Expired
-
2008
- 2008-10-07 CY CY20081101106T patent/CY1108398T1/el unknown
-
2009
- 2009-05-08 JP JP2009113404A patent/JP5133937B2/ja not_active Expired - Lifetime
-
2011
- 2011-07-28 AR ARP110102734A patent/AR082409A2/es active IP Right Grant
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK1K | Patent expired |