KR870001164A - N-아르알킬 피페리딘메탈올 유도체의 제조방법 - Google Patents
N-아르알킬 피페리딘메탈올 유도체의 제조방법 Download PDFInfo
- Publication number
- KR870001164A KR870001164A KR1019860005319A KR860005319A KR870001164A KR 870001164 A KR870001164 A KR 870001164A KR 1019860005319 A KR1019860005319 A KR 1019860005319A KR 860005319 A KR860005319 A KR 860005319A KR 870001164 A KR870001164 A KR 870001164A
- Authority
- KR
- South Korea
- Prior art keywords
- phenyl ring
- formula
- ring bonded
- substituents
- methanol
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
내용 없음.
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (10)
- 하기 일반식 (IIa),(IIb),(IIc) 또는 (IId)의 화합물을 화학적으로 환원시키거나, 하기 일반식(V)의 화합물을 하기 일반식(III)의 반응성 유도체로 알킬화시키거나, 하기 일반식(XI)의 그리그나드 시약을 하기 일반식(VI)의 알데하이드와 반응시킨 다음 반응생성물을 가수분해시킴을 특징으로 하여, 하기 일반식(I)의 화합물, 그의 광학적 이성체 및 그의 약제학적으로 허용되는 염을 제조하는 방법.상기 식에서, 각 R 및 R1은 독립적으로 수소, C1-6알킬, 할로겐, 트리플루오메틸, 하이드록시, C1-6알콕시, 또는 아미노이고, n은 2,3 또는 4이며, X는 반응성 잔기, 바람직하게는 할라이드, 토실레이트, 메실레이트 또는 그의 작용성 등가물이다.
- 제1항에 있어서, n이 2인 방법
- 제1항에 있어서, n이 3인 방법.
- 제1항에 있어서, 알킬에 결합된 페닐환상의 치환체 R 및 R1이 수소인 방법.
- 제4항에 있어서, 메탄올에 결합된 페닐환상의 치환체 R 및 R1이 수소인 방법.
- 제1항에 있어서, 메탄올에 결합된 페닐환상의 치환체 R 및 R1이 메톡시이고, 알킬에 결합된 페닐환상의 치환체 R 및 R1이 수소인 방법.
- 제1항에 있어서, 메탄올에 결합된 페닐환상의 치환체 R이 메톡시이고, 메탄올에 결합된 페닐환상의 치환체 R1, 알킬에 결합된 페닐환상의 치환체 R 및 R1이 각각 수소인 방법.
- 제1항에 있어서, 메탄올에 결합된 페닐환상의 치환체 R 및 R′이 할로겐이고, 알킬에 결합된 페닐환상의 치환체 R 및 R1이 수소인 방법.
- 제1항에 있어서, 메탄올에 결합된 페닐환상의 치환체 R이 메틸이고, 메탄올에 결합된 페닐환상의 치환체 R1, 알킬에 결합된 페닐환상의 치환체 R 및 R1이 각각 수소인 방법.
- 하기 구조식 (VIIIa), (VIIIb), (VIIIc) 또는 (VIIId)의 화합물을 화학적으로 환원시키거나, 하기 구조식(IX)의 화합물을 하기 일반식(X)의 알킬화제로 알킬화시키거나, 하기 구조식(XIII)의 그리그나드 시약을 하기 구조식(XII)의 알데하이드와 반응시킨 다음 반응 생성물을 가수분해시킴을 특징으로 하여, 하기 구조식(VII)의 화합물을 제조하는 방법.상기 식에서, X-치환체는 할라이드, 토실레이트, 메실레이트 또는 그의 작용성 등가물이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US75141985A | 1985-07-02 | 1985-07-02 | |
US751,419 | 1985-07-02 | ||
US751419 | 1985-07-02 |
Publications (2)
Publication Number | Publication Date |
---|---|
KR870001164A true KR870001164A (ko) | 1987-03-11 |
KR900001184B1 KR900001184B1 (ko) | 1990-02-27 |
Family
ID=25021900
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019860005319A KR900001184B1 (ko) | 1985-07-02 | 1986-07-01 | N-아르알킬 피페리딘메탄올 유도체의 제조방법 |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP0208235B1 (ko) |
JP (1) | JPH0655720B2 (ko) |
KR (1) | KR900001184B1 (ko) |
CN (1) | CN1023895C (ko) |
AR (2) | AR241904A1 (ko) |
AT (1) | ATE49403T1 (ko) |
AU (1) | AU590582B2 (ko) |
CA (1) | CA1280421C (ko) |
DE (1) | DE3668167D1 (ko) |
DK (1) | DK174153B1 (ko) |
ES (1) | ES2000299A6 (ko) |
FI (1) | FI84474C (ko) |
GR (1) | GR861699B (ko) |
HU (1) | HU196058B (ko) |
IE (1) | IE58460B1 (ko) |
IL (1) | IL79266A (ko) |
NO (1) | NO167384C (ko) |
NZ (1) | NZ216689A (ko) |
PH (1) | PH22141A (ko) |
PT (1) | PT82890B (ko) |
ZA (1) | ZA864772B (ko) |
Families Citing this family (39)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR910006138B1 (ko) * | 1986-09-30 | 1991-08-16 | 에자이 가부시끼가이샤 | 환상아민 유도체 |
ZA888572B (en) * | 1987-11-23 | 1989-08-30 | Merrell Dow Pharma | Treatment of fibromyalgia |
JPH02138214A (ja) * | 1987-12-10 | 1990-05-28 | Merrell Dow Pharmaceut Inc | 不安を治療する方法 |
US5093341A (en) * | 1987-12-17 | 1992-03-03 | Merrell Dow Pharmaceuticals Inc. | N-aralkyl piperidine derivatives useful as antithrombolytic agents |
ATE102482T1 (de) * | 1988-01-21 | 1994-03-15 | Merrell Dow Pharma | Verwendung von 1,4-disubstituierten-piperidinyl- verbindungen zur herstellung eines arzneimittels zur behandlung von schlaflosigkeit. |
ZA891901B (en) * | 1988-03-17 | 1989-11-29 | Merrell Dow Pharma | Method for the treatment of the extrapyramidal side effects associated with neuroleptic therapy |
JP2969359B2 (ja) * | 1989-01-13 | 1999-11-02 | 武田薬品工業株式会社 | 環状アミン化合物 |
US5032598A (en) * | 1989-12-08 | 1991-07-16 | Merck & Co., Inc. | Nitrogens containing heterocyclic compounds as class III antiarrhythmic agents |
ZA9010081B (en) * | 1989-12-20 | 1991-10-30 | Merrell Dow Pharma | Method for the treatment of glaucoma |
JP2758050B2 (ja) * | 1989-12-27 | 1998-05-25 | 株式会社トクヤマ | 土質安定用薬液およびその注入工法 |
US6004980A (en) * | 1990-06-01 | 1999-12-21 | Merrell Pharmaceuticals, Inc. | (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol |
DE69105501T2 (de) * | 1990-06-01 | 1995-04-13 | Merrell Dow Pharma | (+)-alpha-(2,3 dimethoxyphenyl)-1-[2-(fluorophenyl)ethyl]-4-piperidinmethanol. |
JPH07111050B2 (ja) * | 1990-12-12 | 1995-11-29 | 株式会社親和テクノ | セメントグラウトを用いた地盤注入工法 |
FR2672286B1 (fr) * | 1991-01-31 | 1994-11-18 | Synthelabo | Derives de 1-(4-chlorophenyl)-2-[4-(phenylmethyl)piperidin-1-yl]ethanol, leur preparation et leur application en therapeutique. |
ZA929008B (en) * | 1991-12-13 | 1993-05-21 | Bristol Myers Squibb Co | Piperazinyl- and piperidinyl-cyclohexanols. |
AU4659793A (en) * | 1992-06-30 | 1994-01-24 | United States Of America, Represented By The Secretary, Department Of Health And Human Services, The | Anorectic epinephrine derivatives |
FR2696741B1 (fr) * | 1992-10-12 | 1994-11-25 | Synthelabo | Dérivés de 1-(4-chlorophényl)-2-[4-[(4-fluorophényl)méthyl]piperidin-1-yl] éthanol, leur préparation et leur application en thérapeutique. |
CA2108245A1 (en) * | 1992-11-04 | 1994-05-05 | Gary J. Grover | Method for treating myocardial ischemia employing serotonin receptor antagonists |
EP0661266A1 (en) * | 1993-12-27 | 1995-07-05 | Toa Eiyo Ltd. | Substituted cyclic amine compounds as 5HT2 antagonists |
DE19681115D2 (de) * | 1995-12-20 | 1999-11-25 | Eckhart Pein | Neue 1-Phenylalkyl/Alkylen-4-(.Alpha.-Hydroxydiphenylmethyl)-Piperidin Derivative und ihre Verwendung als Serotonin Antagonisten |
US6028083A (en) * | 1997-07-25 | 2000-02-22 | Hoechst Marion Roussel, Inc. | Esters of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol |
US6713627B2 (en) | 1998-03-13 | 2004-03-30 | Aventis Pharmaceuticals Inc. | Processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol |
TWI249526B (en) * | 1998-03-13 | 2006-02-21 | Aventis Pharma Inc | Novel processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol |
SE9801516D0 (sv) * | 1998-04-30 | 1998-04-30 | Maria Carlsson | M100907/4-Piperidinemethanol derivatives for autism |
DE19934432A1 (de) | 1999-07-22 | 2001-02-01 | Merck Patent Gmbh | Indolderivate |
DE19939756A1 (de) * | 1999-08-21 | 2001-02-22 | Merck Patent Gmbh | Piperidinalkohole |
US7345096B2 (en) | 2002-10-15 | 2008-03-18 | Wyeth | Use of norepinephrine reuptake modulators for preventing and treating vasomotor symptoms |
US7491723B2 (en) | 2003-10-14 | 2009-02-17 | Wyeth | Alkanol and cycloalkanol-amine derivatives and methods of their use |
US7531543B2 (en) | 2003-10-14 | 2009-05-12 | Wyeth | Phenylpiperazine cycloalkanol derivatives and methods of their use |
US7419980B2 (en) | 2003-10-14 | 2008-09-02 | Wyeth | Fused-aryl and heteroaryl derivatives and methods of their use |
US7524846B2 (en) | 2003-10-14 | 2009-04-28 | Wyeth | Arylalkyl- and cycloalkylalkyl-piperazine derivatives and methods of their use |
US7402698B2 (en) | 2003-10-14 | 2008-07-22 | Wyeth | Secondary amino-and cycloamino-cycloalkanol derivatives and methods of their use |
US7550485B2 (en) | 2003-10-14 | 2009-06-23 | Wyeth | Substituted N-heterocycle derivatives and methods of their use |
US7365076B2 (en) | 2003-10-14 | 2008-04-29 | Wyeth | Substituted aryl cycloalkanol derivatives and methods of their use |
EP1691811B1 (en) | 2003-12-11 | 2014-07-23 | Sunovion Pharmaceuticals Inc. | Combination of a sedative and a neurotransmitter modulator, and methods for improving sleep quality and treating depression |
DE102004010132A1 (de) | 2004-02-27 | 2005-09-15 | Merck Patent Gmbh | Piperidinderivate |
US7517899B2 (en) | 2004-03-30 | 2009-04-14 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
US7414052B2 (en) | 2004-03-30 | 2008-08-19 | Wyeth | Phenylaminopropanol derivatives and methods of their use |
WO2006029182A2 (en) * | 2004-09-07 | 2006-03-16 | The La Jolla Institute For Molecular Medicine | Use of mdl-100,907 for treatment of allergic and eosinophil mediated diseases |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3100775A (en) * | 1959-04-01 | 1963-08-13 | Searle & Co | alpha-phenyl(pyridyl or piperidyl)alkyl esters of (chloro or lower alkoxy)-benzoic acids and congeners |
ZA717147B (en) * | 1970-11-27 | 1972-07-26 | Richardson Merrell Inc | 4-(4-(alpha-hydroxybenzyl)piperidino)-4'-fluorobutyrophenone derivatives |
SE7409245L (ko) * | 1973-07-19 | 1975-01-20 | Robins Co Inc A H | |
FR2534580A1 (fr) * | 1982-10-13 | 1984-04-20 | Synthelabo | Derives de phenyl-1 piperidino-2 propanol, leur preparation, et medicaments qui les contiennent |
KR910006138B1 (ko) * | 1986-09-30 | 1991-08-16 | 에자이 가부시끼가이샤 | 환상아민 유도체 |
-
1986
- 1986-06-26 CA CA000512511A patent/CA1280421C/en not_active Expired - Lifetime
- 1986-06-26 ZA ZA864772A patent/ZA864772B/xx unknown
- 1986-06-27 PH PH33962A patent/PH22141A/en unknown
- 1986-06-27 NZ NZ216689A patent/NZ216689A/xx unknown
- 1986-06-27 IL IL79266A patent/IL79266A/xx not_active IP Right Cessation
- 1986-06-27 AU AU59318/86A patent/AU590582B2/en not_active Expired
- 1986-06-30 GR GR861699A patent/GR861699B/el unknown
- 1986-07-01 AT AT86108941T patent/ATE49403T1/de not_active IP Right Cessation
- 1986-07-01 IE IE177186A patent/IE58460B1/en not_active IP Right Cessation
- 1986-07-01 KR KR1019860005319A patent/KR900001184B1/ko not_active IP Right Cessation
- 1986-07-01 JP JP61152855A patent/JPH0655720B2/ja not_active Expired - Lifetime
- 1986-07-01 NO NO862661A patent/NO167384C/no not_active IP Right Cessation
- 1986-07-01 ES ES8600071A patent/ES2000299A6/es not_active Expired
- 1986-07-01 FI FI862801A patent/FI84474C/fi not_active IP Right Cessation
- 1986-07-01 HU HU862738A patent/HU196058B/hu unknown
- 1986-07-01 EP EP86108941A patent/EP0208235B1/en not_active Expired - Lifetime
- 1986-07-01 DK DK198603123A patent/DK174153B1/da not_active IP Right Cessation
- 1986-07-01 PT PT82890A patent/PT82890B/pt unknown
- 1986-07-01 CN CN86104408A patent/CN1023895C/zh not_active Expired - Lifetime
- 1986-07-01 DE DE8686108941T patent/DE3668167D1/de not_active Expired - Lifetime
- 1986-07-02 AR AR86304417A patent/AR241904A1/es active
-
1990
- 1990-04-06 AR AR90316571A patent/AR242184A1/es active
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