KR830007552A - 3-(피리드-3- 또는 -4-일알킬) 인돌의 제조방법 - Google Patents

3-(피리드-3- 또는 -4-일알킬) 인돌의 제조방법 Download PDF

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KR830007552A
KR830007552A KR1019810004911A KR810004911A KR830007552A KR 830007552 A KR830007552 A KR 830007552A KR 1019810004911 A KR1019810004911 A KR 1019810004911A KR 810004911 A KR810004911 A KR 810004911A KR 830007552 A KR830007552 A KR 830007552A
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compound
formula
alkyl
coo
cooh
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KR1019810004911A
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에드워드 크로쓰 피터
피터 딕킨슨 로저
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윌리암 존 윌슨
화이자 코포레이숀
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Publication of KR830007552A publication Critical patent/KR830007552A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

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  • Organic Chemistry (AREA)
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  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

내용 없음

Description

3-(피리드-3-또는-4-일알킬) 인돌의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 염기존재하에 일반식(Ⅱ) 화합물을 일반식(Ⅲ) 또는 일반식(Ⅳ)의 알킬화제와 반응시키고 경우에 따라서 다음 (a) 내지 (g)공정중 하나이상을 실시함을 특징으로 하는 일반식(Ⅰ) 화합물 및 그의 약학적으로 허용되는 염의 제조방법.
    (상기 구조식에서,
    R1은 수소, C1-C4알킬, C3-C7싸이클로알킬 또는 페닐이고,
    R2는 수소, C1-C4알킬, C1-C4알콕시 또는 할로이고,
    R3는 수소 또는 C1-C4알킬이고,
    X는 -(CH2)n- (이때 n은 1,2 또는 3),또는이고,
    Y는 -COOH, -COO(C4-C1알킬), -CONH2, -CN 또는 5-테트라졸릴이고,
    Z는 3- 또는 4-피리딜이고,
    Hal은 Cl,Br 또는 I이고,
    R4는 H 또는 CH3이고,
    Y1은 -CH 또는 -COO(C1-C4알킬)이다.
    (a) Y가 -COO(C1-C4알킬)인 일반식(Ⅰ)화합물을 가수분해시켜 Y가 -COOH인 일반식(Ⅰ)화합물로 전환시킴:
    (b) Y가 -COOH1인 일반식(Ⅰ) 화합물을 산할라이드 또는 이미다졸리드로 만든 다음 암모니아와 반응시켜 Y가 -CONH2인 일반식(Ⅰ) 화합물로 전환시킴;
    (C) Y가 -COOH인 일반식(Ⅰ) 화합물을 에스테르화시켜 Y가 -COO(C1-C4알킬)인 일반식(Ⅰ) 화합물로 전환시킴;
    (d) Y가 -CN인 일반식(Ⅰ) 화합물을 각각 약한 또는 강한 가수분해를 시켜 Y가 -CONH2또는 -COOH인 일반식(Ⅰ) 화합물로 전환시킴;
    (e) Y가 -CN인 일반식(Ⅰ) 화합물을 소듐아지드 및 염화암모늄과 반응시켜 Y가 5-테트라졸릴인 일반식(Ⅰ) 화합물로 전환시킴;
    (f) Y가 -COO(C1-C4알킬)인 일반식(Ⅰ) 화합물을 암모니아와 반응시켜 Y가 -CONH2인 일반식(Ⅰ) 화합물로 전환시킴; 및
    (g) 일반식(Ⅰ) 화합물을 통상의 공정에 따라 그의 약학적으로 허용되는 염으로 전환시킴.
  2. 특허청구범위 제1항에 있어서, 알킬화제로서 일반식(Ⅲ) 화합물을 사용하고 염기로서 소튬하이드리드를 사용함을 특징으로 하는 방법.
  3. 특허청구범위 제1항에 있어서, 알킬화제로서 일반식(Ⅳ) 화합물을 사용하고 염기로서 벤질트리메틸 암모늄하이드록사이드를 사용함을 특징으로 하는 방법.
  4. 특허청구범위 제1항 또는 2항에 있어서, 소듐하이드리드 존재하에 2-메틸-3-(3-피리딜메틸)인돌을 에틸브로모아세테이트와 반응시킨 다음 생성된 에스테르를 알카리 가수분해시켜 2-[2-메틸-3-(3-피리딜메틸) 인돌-1-일] 초산을 제조함을 특징으로 하는 방법.
  5. 특허청구범위 제1항 또는 2항에 있어서, 소듐하이드리드 존재하에 2,5-디메틸-3-(3-피리딜메틸)인돌을 에틸브로모아세테이트와 반응시킨 다음 생성된 에스테르를 알칼리 가수분해시켜 2-[2,5-디메틸-3-(3-피리딜메틸)인돌-1-일]초산을 제조함을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810004911A 1980-12-15 1981-12-14 3-(피리드-3- 또는 -4-일알킬) 인돌의 제조방법 KR830007552A (ko)

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GB8040081 1980-12-15
GB8040081 1980-12-15

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KR830007552A true KR830007552A (ko) 1983-10-21

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US (1) US4363912A (ko)
EP (1) EP0054417B1 (ko)
JP (1) JPS57181082A (ko)
KR (1) KR830007552A (ko)
AR (1) AR229110A1 (ko)
AU (1) AU525296B2 (ko)
CA (1) CA1143737A (ko)
CS (1) CS228527B2 (ko)
DD (1) DD202290A5 (ko)
DE (1) DE3167879D1 (ko)
DK (1) DK552581A (ko)
ES (1) ES8308872A1 (ko)
FI (1) FI814003L (ko)
GR (1) GR76355B (ko)
IE (1) IE51949B1 (ko)
IL (1) IL64534A0 (ko)
NO (1) NO814264L (ko)
PH (1) PH17576A (ko)
PL (1) PL133634B1 (ko)
PT (1) PT74123B (ko)
YU (1) YU293481A (ko)
ZA (1) ZA818665B (ko)

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CS229934B2 (en) * 1981-07-07 1984-07-16 Pfizer Production method subst.indolylacryte acid derivative
US4460777A (en) * 1981-11-19 1984-07-17 Ciba-Geigy Corporation N-Substituted-2-pyridylindoles
US4478842A (en) * 1981-11-19 1984-10-23 Ciba-Geigy Corporation N-Substituted-2-pyridylindoles
US4536505A (en) * 1983-05-17 1985-08-20 Ciba-Geigy Corporation Certain N-(pyridyl) indoles
US4511573A (en) * 1983-05-17 1985-04-16 Ciba-Geigy Corporation 3-Substituted-2-(heteroaryl) indoles
GB8524157D0 (en) * 1984-10-19 1985-11-06 Ici America Inc Heterocyclic amides
US4609733A (en) * 1984-12-27 1986-09-02 Ciba-Geigy Corporation 3-keto-substituted-N-pyridylindoles
GB8609175D0 (en) * 1986-04-15 1986-05-21 Ici America Inc Heterocyclic carboxamides
KR100584650B1 (ko) * 1998-03-31 2006-05-30 디 인스티튜트스 포 파마슈티컬 디스커버리, 엘엘씨 치환된 인돌알칸산
TNSN99224A1 (fr) * 1998-12-01 2005-11-10 Inst For Pharm Discovery Inc Methodes de reduction des niveaux de glucose et triglyceride en serum et pour suppression de l'antigenese utilisant les acides la indolealkanoique
AU2001232785A1 (en) * 2000-01-14 2001-07-24 The Institutes For Pharmaceutical Discovery, Llc Methods for lowering uric acid levels
CA2509170A1 (en) * 2002-12-10 2004-06-24 Wyeth Substituted 3-alkyl and 3-arylalkyl 1h-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (pai-1)
GB0324763D0 (en) * 2003-10-23 2003-11-26 Oxagen Ltd Use of compounds in therapy
JP5270542B2 (ja) 2006-07-22 2013-08-21 オキサジェン リミテッド Ｃｒｔｈ２アンタゴニスト活性を有する化合物
RU2010112275A (ru) * 2007-09-24 2011-11-10 Аллерган, Инк. (Us) Индольные соединения, содержащие арильные или гетероарильные группы, обладющие биологической активностью рецептора сфингозин-1-фосфата (с1ф)
US7750027B2 (en) 2008-01-18 2010-07-06 Oxagen Limited Compounds having CRTH2 antagonist activity
CN101932571B (zh) * 2008-01-18 2014-04-23 奥克萨根有限公司 具有crth2拮抗活性的化合物
WO2009093026A1 (en) 2008-01-22 2009-07-30 Oxagen Limited Compounds having crth2 antagonist activity
WO2009093029A1 (en) * 2008-01-22 2009-07-30 Oxagen Limited Compounds having crth2 antagonist activity
GB201322273D0 (en) 2013-12-17 2014-01-29 Atopix Therapeutics Ltd Process
GB201407807D0 (en) * 2014-05-02 2014-06-18 Atopix Therapeutics Ltd Polymorphic form
GB201407820D0 (en) * 2014-05-02 2014-06-18 Atopix Therapeutics Ltd Polymorphic form

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FR5173M (ko) * 1966-02-11 1967-06-19
FR7337M (ko) * 1968-01-11 1969-10-13
GB2045244B (en) 1979-03-07 1983-01-26 Pfizer Ltd 3-1-(imidazolylalkyl) indoles
US4322533A (en) * 1980-03-17 1982-03-30 Lesher George Y 1H-Indole-2,3-dione derivatives

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FI814003L (fi) 1982-06-16
EP0054417B1 (en) 1984-12-19
ES507960A0 (es) 1983-10-01
DE3167879D1 (en) 1985-01-31
DD202290A5 (de) 1983-09-07
PT74123A (en) 1982-01-01
IL64534A0 (en) 1982-03-31
AU7848881A (en) 1982-06-24
CA1143737A (en) 1983-03-29
AU525296B2 (en) 1982-10-28
US4363912A (en) 1982-12-14
IE812928L (en) 1982-06-15
EP0054417A1 (en) 1982-06-23
NO814264L (no) 1982-06-16
AR229110A1 (es) 1983-06-15
IE51949B1 (en) 1987-04-29
CS228527B2 (en) 1984-05-14
PL234253A1 (en) 1983-05-23
JPS57181082A (en) 1982-11-08
ZA818665B (en) 1982-10-27
PT74123B (en) 1983-12-19
GR76355B (ko) 1984-08-06
YU293481A (en) 1984-10-31
ES8308872A1 (es) 1983-10-01
PH17576A (en) 1984-10-01
PL133634B1 (en) 1985-06-29
DK552581A (da) 1982-06-16

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