KR860008207A - 신규 안드로스탄-17β- 카르복실산 에스테르의 제조 방법 - Google Patents
신규 안드로스탄-17β- 카르복실산 에스테르의 제조 방법 Download PDFInfo
- Publication number
- KR860008207A KR860008207A KR1019860002522A KR860002522A KR860008207A KR 860008207 A KR860008207 A KR 860008207A KR 1019860002522 A KR1019860002522 A KR 1019860002522A KR 860002522 A KR860002522 A KR 860002522A KR 860008207 A KR860008207 A KR 860008207A
- Authority
- KR
- South Korea
- Prior art keywords
- group
- hydrogen
- atom
- chlorine
- compound
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title claims 2
- PBXJGQQGODZSQR-CWQDBKDDSA-N (8r,9s,10s,13s,14s,17s)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthrene-17-carboxylic acid Chemical compound C1CCC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(O)=O)[C@@H]4[C@@H]3CCC21 PBXJGQQGODZSQR-CWQDBKDDSA-N 0.000 title 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical compound BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 8
- 229910052801 chlorine Inorganic materials 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical compound ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 239000011737 fluorine Substances 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 229930195733 hydrocarbon Natural products 0.000 claims 2
- 150000002430 hydrocarbons Chemical class 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- -1 nitro, carboxy Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 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
- C07J41/0038—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
-
- 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
-
- 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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (3)
- 다음 일반식(Ⅱ)의 화합물 및 그 염을 다음 일반식(Ⅲ)의 화합물과 반응시킴을 특징으로 하는 하기 일반식(Ⅰ)의 화합물 또는 그 입체이성질체의 제조 방법.상기 식중,X1은 수소, 염소, 브롬 또는 불소 원자이고,X2는 수소, 염소, 브롬 또는 불소 원자이고,R1은 β-히드록시기, β-염소 원자 또는 옥소기이고,R2는 수소 원자, 메틸렌기 또는 α-메틸기 또는 β-메틸기이고,R3는 수소 원자, 또는 탄소 원자 수가 1 내지 8개인 알칸오일기이고,R4는 수소 원자, (C1-C5) 알킬기 또는 페닐기이고,R5는 수소 원자, (C1-C5) 알킬기 또는 페닐기이고,Y는 CR7R8,O,S 또는 NR9기 [여기에서, R7,R8및 R9는 수소, 탄소 원자 수가 1-8개인 직쇄 또는 측쇄 탄화 수소 또는 페닐기로부터 선택됨]이고,R6은 수소 원자, 메틸기, 페닐, 알케닐기 또는 시클로알케닐기(페닐, 알케닐 또는 시클로알케닐기는 알킬, 니트로, 카르복시, 알콕시, 할로겐, 시아노, 카르브알콕시 및 트리플루오로메틸기에 의해 임의로 치환됨), (C1-C5) 알킬기(이 알킬기는 1개 이상의 할로겐 원자에 의해 치환됨), 포화카르보시클릭, 불포화카르보시클릭 또는 헤테로시클릭(O,S,N) 고리계(이 고리계는 고리계 중에 3-10 원자를 함유함), C5알킬기[이 알킬기는 1 또는 2개의 알리시클릭 또는 방향족 3,4,5 또는 6원 고리계, 또는 1,2 또는 3개의 직쇄 또는 측쇄, 포화 또는 불포화탄화수소(이 탄화수소는 탄소 원자 수가 1 내지 18개임)에 의해 임의로 치환됨]이고,는 단일 또는 이중 결합이고,Z는 할로겐 원자 또는 기능적으로 동일한 기이다.
- 제 1항에 있어서, 일반식(Ⅰ)의 화합물이X1가 불소 또는 염소 원자이고,X2가 불소 또는 염소 원자이고,R1이 β-히드록시기이고,R3가 아세틸기, 프로피오닐기, 부티릴기, 또는 발레로일기이고,R4/R5가 수소/메틸기 또는 메틸기/수소이고,Y가 0이고,R6이 탄소 원자 수가 1-5인 알킬기이고,가 이중 결합인 것을 특징으로 하는 방법.
- 제 1항에 있어서, 일반식(Ⅰ)의 화합물이 하기 일반식(Ⅱ)의 화합물 또는 그 염류로부터 제조됨을 특징으로 하는 방법.상기 식중,X1은 수소, 염소, 브롬 또는 불소 원자이고,X2는 수소, 염소, 브롬 또는 불소 원자이고,R1은 β-히드록시기, β-염소 원자 또는 옥소기이고,R2는 수소 원자, 메틸렌기 또는 α-메틸기 또는 β-메틸기이고,R3는 수소 원자 또는 탄소 원자 수가 1 내지 8개인 아실기이고,는 단일 또는 이중 결합이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE8501692-1 | 1985-04-04 | ||
| SE8501692A SE8501692D0 (sv) | 1985-04-04 | 1985-04-04 | Novel androstane-17beta-carboxylic acid esters |
| SE8502932-0 | 1985-06-13 | ||
| SE8502932A SE8502932D0 (sv) | 1985-06-13 | 1985-06-13 | Novel androstane-17beta-carboxylic acid esters |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR860008207A true KR860008207A (ko) | 1986-11-14 |
Family
ID=26658930
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019860002522A KR860008207A (ko) | 1985-04-04 | 1986-04-03 | 신규 안드로스탄-17β- 카르복실산 에스테르의 제조 방법 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US4804656A (ko) |
| EP (1) | EP0200692B1 (ko) |
| JP (1) | JPH0764869B2 (ko) |
| KR (1) | KR860008207A (ko) |
| CN (1) | CN86102263A (ko) |
| AR (1) | AR243535A1 (ko) |
| AT (1) | ATE67210T1 (ko) |
| AU (1) | AU594330B2 (ko) |
| CA (1) | CA1278293C (ko) |
| CS (1) | CS266580B2 (ko) |
| DE (1) | DE3681334D1 (ko) |
| DK (1) | DK165880C (ko) |
| EG (1) | EG18042A (ko) |
| ES (1) | ES8800261A1 (ko) |
| FI (1) | FI86190C (ko) |
| GR (1) | GR860901B (ko) |
| HU (1) | HU200782B (ko) |
| IE (1) | IE58309B1 (ko) |
| IL (1) | IL78144A0 (ko) |
| MY (1) | MY102057A (ko) |
| NO (1) | NO165679C (ko) |
| NZ (1) | NZ215587A (ko) |
| PH (2) | PH22578A (ko) |
| PL (1) | PL148734B1 (ko) |
| PT (1) | PT82339B (ko) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5252319A (en) * | 1990-06-12 | 1993-10-12 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5256408A (en) * | 1990-06-12 | 1993-10-26 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5209926A (en) * | 1990-06-12 | 1993-05-11 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5124154A (en) * | 1990-06-12 | 1992-06-23 | Insite Vision Incorporated | Aminosteroids for ophthalmic use |
| US5652363A (en) * | 1995-10-05 | 1997-07-29 | C.D. Searle & Co. | Pyrido-1,4-oxazinylalkyl-benzamide derivatives |
| CA2241728A1 (en) | 1995-12-29 | 1997-07-10 | Panayiotis Alexandrou Procopiou | Lactone derivatives of 17.beta.-carboxy, carbothio and amide androstane derivatives |
| WO1999001467A2 (en) * | 1997-06-30 | 1999-01-14 | Glaxo Group Limited | Therapeutically active compounds with low systemic activity due to reduce half life |
| US7186855B2 (en) | 2001-06-11 | 2007-03-06 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US7232924B2 (en) | 2001-06-11 | 2007-06-19 | Xenoport, Inc. | Methods for synthesis of acyloxyalkyl derivatives of GABA analogs |
| US6818787B2 (en) | 2001-06-11 | 2004-11-16 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
| US8048917B2 (en) | 2005-04-06 | 2011-11-01 | Xenoport, Inc. | Prodrugs of GABA analogs, compositions and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3828080A (en) * | 1972-01-20 | 1974-08-06 | Glaxo Lab Ltd | Androstane-17beta-carboxylic acids and processes for the preparation thereof |
| GB1438940A (en) * | 1972-07-19 | 1976-06-09 | Glaxo Lab Ltd | 17beta-haloalkoxycarbonyl-17alpha-oxysteroids |
| GB1517278A (en) * | 1974-08-30 | 1978-07-12 | Glaxo Lab Ltd | Alkyl and haloalkyl androsta-1,4,15-triene and-4,15-diene-17beta-carboxylates |
| CH628355A5 (de) * | 1976-02-24 | 1982-02-26 | Ciba Geigy Ag | Verfahren zur herstellung neuer androstadien-17beta-carbonsaeuren und ihrer ester und salze. |
| US4188385A (en) * | 1978-04-05 | 1980-02-12 | Syntex (U.S.A.) Inc. | Thioetianic acid derivatives |
| US4198336A (en) * | 1978-04-05 | 1980-04-15 | Syntex (U.S.A.) Inc. | Chemical process for preparing androsta-4-ene 17α-carboxylic acids |
| ZA814440B (en) * | 1980-07-10 | 1982-10-27 | Otsuka Pharma Co Ltd | Soft steroids having anti-inflammatory activity |
| SE449106B (sv) * | 1980-07-10 | 1987-04-06 | Otsuka Pharma Co Ltd | Steroid med anti-inflammatorisk verkan samt komposition innehallande denna |
| US4710495A (en) * | 1980-07-10 | 1987-12-01 | Otsuka Pharmaceutical Co., Ltd. | Soft steroids having anti-inflammatory activity |
| ZA817929B (en) * | 1980-12-22 | 1982-10-27 | Upjohn Co | 5alpha-and 5beta-androstane-17beta-carboxylates |
| US4607028A (en) * | 1983-08-18 | 1986-08-19 | Ciba-Geigy Corporation | Novel carboxylic acid esters |
-
1986
- 1986-03-14 IL IL78144A patent/IL78144A0/xx not_active IP Right Cessation
- 1986-03-24 PH PH33572A patent/PH22578A/en unknown
- 1986-03-25 DK DK138486A patent/DK165880C/da not_active IP Right Cessation
- 1986-03-25 FI FI861274A patent/FI86190C/fi not_active IP Right Cessation
- 1986-03-26 AR AR86303485A patent/AR243535A1/es active
- 1986-04-01 EP EP86850113A patent/EP0200692B1/en not_active Expired - Lifetime
- 1986-04-01 DE DE8686850113T patent/DE3681334D1/de not_active Expired - Lifetime
- 1986-04-01 AT AT86850113T patent/ATE67210T1/de not_active IP Right Cessation
- 1986-04-02 AU AU55566/86A patent/AU594330B2/en not_active Ceased
- 1986-04-02 CS CS862327A patent/CS266580B2/cs unknown
- 1986-04-02 NZ NZ215587A patent/NZ215587A/xx unknown
- 1986-04-03 ES ES553674A patent/ES8800261A1/es not_active Expired
- 1986-04-03 CA CA000505743A patent/CA1278293C/en not_active Expired - Fee Related
- 1986-04-03 JP JP61075678A patent/JPH0764869B2/ja not_active Expired - Lifetime
- 1986-04-03 NO NO861312A patent/NO165679C/no unknown
- 1986-04-03 HU HU861424A patent/HU200782B/hu not_active IP Right Cessation
- 1986-04-03 US US06/847,933 patent/US4804656A/en not_active Expired - Lifetime
- 1986-04-03 KR KR1019860002522A patent/KR860008207A/ko not_active Application Discontinuation
- 1986-04-03 IE IE87886A patent/IE58309B1/en not_active IP Right Cessation
- 1986-04-04 CN CN198686102263A patent/CN86102263A/zh active Pending
- 1986-04-04 PT PT82339A patent/PT82339B/pt not_active IP Right Cessation
- 1986-04-04 GR GR860901A patent/GR860901B/el unknown
- 1986-04-04 PL PL1986258776A patent/PL148734B1/pl unknown
- 1986-04-30 EG EG184/86A patent/EG18042A/xx active
-
1987
- 1987-09-28 MY MYPI87001993A patent/MY102057A/en unknown
-
1988
- 1988-06-13 PH PH37056A patent/PH25535A/en unknown
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