KR890005141A - 안드로스타-1,4-디엔-3,17-디온의 메틸렌 유도체의 제조방법 - Google Patents
안드로스타-1,4-디엔-3,17-디온의 메틸렌 유도체의 제조방법 Download PDFInfo
- Publication number
- KR890005141A KR890005141A KR1019880011641A KR880011641A KR890005141A KR 890005141 A KR890005141 A KR 890005141A KR 1019880011641 A KR1019880011641 A KR 1019880011641A KR 880011641 A KR880011641 A KR 880011641A KR 890005141 A KR890005141 A KR 890005141A
- Authority
- KR
- South Korea
- Prior art keywords
- formula
- compound
- hydrogen
- alkyl
- formaldehyde source
- Prior art date
Links
Classifications
-
- 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
-
- 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
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
-
- 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
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
- C07J1/0022—Androstane 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
- C07J75/00—Processes for the preparation of steroids in general
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
- Saccharide Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (5)
- 일반식(Ⅱ)의 화합물을 포름알데히드 공급원 및 일반식(Ⅲ)의 아민, 또는 이의 염과 반응시켜 일반식(Ⅳ)의 화합물을 수득하고, 수득한 일반식(Ⅳ)의 화합물을 그 자체가 공지된 방법으로 산화시킴을 특징으로 하여, 일반식(Ⅰ)의 화합물을 제조하는 방법.상기식에서 R1,및 R3는 각각 독립적으로, 수소 또는 C1내지 C6알킬이고; R2는 수소, 할로겐 또는 C1내지 C6알킬이며; R4는 수소 또는 불소이고; R그룹은 각각 동일하거나 상이할 수 있으며, 저급알킬이다.
- 제1항에 있어서, 일반식(Ⅱ)의 화합물을 이소펜탄올 중, 적어도 130℃의 온도에서 포름알데히드 공급원 및 할로겐화수소산과 일반식(Ⅲ)의 아민 사이에서 형성된 염과 반응시키는 방법.
- 제1항에 있어서, 일반식(Ⅱ)의 화합물을, 할로겐화 수소산과 일반식(Ⅲ)의 아민 사이에서 형성된 염을 포름알데히드 공급원과 반응시켜 수득한 만니히(Mannich)염과 반응시키는 방법.
- 제1항 내지 3항중 어느 한 항에 있어서, 포름알데히드 공급원이 파라포름알데히드인 방법.
- 약제학적으로 허용되는 담체 또는 희석제 및 활성소로서 제1항에 청구된 방법에 따라 제조된 일반식(Ⅰ)의 화합물을 함유함을 특징으로 하는 약제학적 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB878721383A GB8721383D0 (en) | 1987-09-11 | 1987-09-11 | Preparation of methylene derivatives |
GB8721383 | 1987-09-11 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR890005141A true KR890005141A (ko) | 1989-05-13 |
KR970005315B1 KR970005315B1 (ko) | 1997-04-15 |
Family
ID=10623618
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880011641A KR970005315B1 (ko) | 1987-09-11 | 1988-09-09 | 안드로스타-1,4-디엔-3,17-디온의 메틸렌 유도체의 제조방법 |
Country Status (16)
Country | Link |
---|---|
US (1) | US4876045A (ko) |
EP (1) | EP0307134B1 (ko) |
JP (1) | JP2791046B2 (ko) |
KR (1) | KR970005315B1 (ko) |
AT (1) | ATE78488T1 (ko) |
AU (1) | AU602608B2 (ko) |
CA (1) | CA1316914C (ko) |
DE (1) | DE3872995T2 (ko) |
ES (1) | ES2051858T3 (ko) |
FI (1) | FI884087A (ko) |
GB (1) | GB8721383D0 (ko) |
GR (1) | GR3005296T3 (ko) |
HU (1) | HU199156B (ko) |
IL (1) | IL87657A (ko) |
SU (1) | SU1681731A3 (ko) |
UA (1) | UA6044A1 (ko) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9201224D0 (en) * | 1992-01-21 | 1992-03-11 | Erba Carlo Spa | Difluoromethylenandrostenone derivatives and process for their preparation |
WO2001004342A1 (en) * | 1999-07-07 | 2001-01-18 | Pharmacia & Upjohn Company | Process to prepare exemestane |
CN1304413C (zh) * | 2002-10-24 | 2007-03-14 | 上海华拓医药科技发展有限公司 | 一种抗癌药物依西美坦制备方法 |
EP1709062B9 (en) | 2004-01-16 | 2013-02-13 | Cedarburg Pharmaceuticals, Inc. | Exemestane and its intermediates and methods of making the same |
US10174070B2 (en) | 2005-09-30 | 2019-01-08 | Endece Llc | 6-substituted estradiol derivatives and methods of use |
US20070225354A1 (en) * | 2006-03-21 | 2007-09-27 | Eric Marchewitz | Use of dihydrolipoamide for enhancing physical performance |
US7569719B1 (en) * | 2006-10-25 | 2009-08-04 | Loctite (R&D) Limited | Method of preparing electron deficient olefins |
US20080275259A1 (en) * | 2007-05-04 | 2008-11-06 | Scinopharm Taiwan, Ltd | Process for preparing aromatase inhibitors |
SI2170329T1 (sl) * | 2007-06-25 | 2015-03-31 | Scinopharm Taiwan Ltd. | Postopek za izdelavo kristaliničnega polimorfa 7-etil-10-hidroksikamptotecina |
US20090018356A1 (en) * | 2007-06-25 | 2009-01-15 | Scinopharm Taiwan Ltd. | Crystalline polymorph of exemestane |
US8053589B1 (en) * | 2007-10-24 | 2011-11-08 | Henkel Ireland Limited | Imines and methods of preparing electron deficient olefins using such novel imines |
US8686105B2 (en) | 2007-10-24 | 2014-04-01 | Henkel IP & Holding GmbH | Adhesive systems using imines and salts thereof, precursors to electron deficient olefins and coreactants therefor |
US7973119B1 (en) | 2007-10-24 | 2011-07-05 | Loctite (R&D) Limited | Adhesive systems using imines and salts thereof and precursurs to electron deficient olefins |
WO2009053482A2 (en) * | 2007-10-24 | 2009-04-30 | Loctite (R & D) Limited | Activated methylene reagents and curable compositions prepared therefrom |
CA2703603A1 (en) * | 2007-10-24 | 2009-04-30 | Loctite (R&D) Limited | Electron deficient olefins |
US10196471B1 (en) | 2008-10-24 | 2019-02-05 | Henkel IP & Holding GmbH | Curable composition having an electron deficient olefin |
US8399698B1 (en) | 2008-10-24 | 2013-03-19 | Henkel Ireland Limited | Substituted activated methylene reagents and methods of using such reagents to form electron deficient olefins |
ES2587977T3 (es) | 2009-05-01 | 2016-10-28 | Celloxess Llc | Tratamiento de la infertilidad masculina secundaria al estrés oxidativo de esperma |
JP5981434B2 (ja) | 2010-09-14 | 2016-08-31 | エンディース エルエルシーEndece,Llc | 選択的ER−βアゴニストとしての6−置換デメチル−エストラジオール誘導体 |
CN105085599A (zh) * | 2014-05-16 | 2015-11-25 | 绍兴文理学院 | 一种依西美坦中间体17,17-乙二氧基-6-亚甲基雄甾-1,4-二烯-3-酮及其制备方法和应用 |
CN105294807A (zh) * | 2014-06-26 | 2016-02-03 | 浙江医药股份有限公司新昌制药厂 | 一种依西美坦中间体肟化合物及其制备方法和应用 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3004508C2 (de) * | 1980-02-05 | 1981-12-10 | Schering Ag Berlin Und Bergkamen, 1000 Berlin | Verfahren zur Herstellung von 6-Methylensteroiden |
GB8517360D0 (en) * | 1985-07-09 | 1985-08-14 | Erba Farmitalia | Substituted androsta-1,4-diene-3,17-diones |
-
1987
- 1987-09-11 GB GB878721383A patent/GB8721383D0/en active Pending
-
1988
- 1988-09-01 DE DE8888308103T patent/DE3872995T2/de not_active Expired - Lifetime
- 1988-09-01 AT AT88308103T patent/ATE78488T1/de active
- 1988-09-01 ES ES88308103T patent/ES2051858T3/es not_active Expired - Lifetime
- 1988-09-01 EP EP88308103A patent/EP0307134B1/en not_active Expired - Lifetime
- 1988-09-02 IL IL87657A patent/IL87657A/xx not_active IP Right Cessation
- 1988-09-06 FI FI884087A patent/FI884087A/fi not_active Application Discontinuation
- 1988-09-07 AU AU21980/88A patent/AU602608B2/en not_active Expired
- 1988-09-08 JP JP63225508A patent/JP2791046B2/ja not_active Expired - Lifetime
- 1988-09-09 CA CA000576897A patent/CA1316914C/en not_active Expired - Lifetime
- 1988-09-09 SU SU884356486A patent/SU1681731A3/ru active
- 1988-09-09 HU HU884665A patent/HU199156B/hu unknown
- 1988-09-09 KR KR1019880011641A patent/KR970005315B1/ko not_active IP Right Cessation
- 1988-09-09 UA UA4356486A patent/UA6044A1/uk unknown
- 1988-09-12 US US07/242,854 patent/US4876045A/en not_active Expired - Lifetime
-
1992
- 1992-07-29 GR GR920401628T patent/GR3005296T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
GB8721383D0 (en) | 1987-10-21 |
KR970005315B1 (ko) | 1997-04-15 |
JP2791046B2 (ja) | 1998-08-27 |
SU1681731A3 (ru) | 1991-09-30 |
CA1316914C (en) | 1993-04-27 |
UA6044A1 (uk) | 1994-12-29 |
ES2051858T3 (es) | 1994-07-01 |
US4876045A (en) | 1989-10-24 |
HU199156B (en) | 1990-01-29 |
FI884087A0 (fi) | 1988-09-06 |
IL87657A0 (en) | 1989-02-28 |
ATE78488T1 (de) | 1992-08-15 |
DE3872995T2 (de) | 1992-12-10 |
FI884087A (fi) | 1989-03-12 |
DE3872995D1 (de) | 1992-08-27 |
IL87657A (en) | 1993-02-21 |
AU602608B2 (en) | 1990-10-18 |
GR3005296T3 (ko) | 1993-05-24 |
JPH01104095A (ja) | 1989-04-21 |
EP0307134B1 (en) | 1992-07-22 |
AU2198088A (en) | 1989-03-16 |
EP0307134A1 (en) | 1989-03-15 |
HUT48273A (en) | 1989-05-29 |
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