KR830007551A - 1-카복시 알카노일 인돌린-2-카복실산 유도체의 제조방법 - Google Patents

1-카복시 알카노일 인돌린-2-카복실산 유도체의 제조방법 Download PDF

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KR830007551A
KR830007551A KR1019810004109A KR810004109A KR830007551A KR 830007551 A KR830007551 A KR 830007551A KR 1019810004109 A KR1019810004109 A KR 1019810004109A KR 810004109 A KR810004109 A KR 810004109A KR 830007551 A KR830007551 A KR 830007551A
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hydrogen
compound
formula
indolin
carboxy
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KR1019810004109A
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KR890000662B1 (ko
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그룬펠드 로버트
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아놀드 자일러,에른스트 알테르
시바-가이기 에이지
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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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • 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
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Treatment Of Liquids With Adsorbents In General (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

내용 없음

Description

1-카복시 알카노일 인돌린-2-카복실산 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. (1) 다음 일반식(Ⅲ) 화합물 또는 이의 산 또는 아미노 유도체를 다음 일반식(Ⅳ) 화합물의 반응성의 작용기 유도체와 축합시키거나
    (2) 다음 일반식(Ⅴ)의 화합물을 가수분해 또는 가열콜분해하거나
    (3) 다음 일반식(Ⅵ) 화합물 또는 이의 산 또는 아미노유도체에서 인돌 잔가를 인돌린 잔기로 수소화하여 다음 일반식(I)의 1-카복시-(알카노일 또는 아르알카노일)-인돌린-2-카복실산 유도체 및 이들의 염을 제조하는 방법.
    상기 일반식에서
    Ph는 비치환된 1,2-페닐렌 또는 저급알킬, 저급알콕시, 저급알킬렌디옥시, 하이드록시, 할로게노또는 트리플루오로 메틸에서 선택된 1내지 3의 같거나 다른 그룹으로 치환된 1,2-페닐렌이고
    R1, R2및 R3는 각기 수소 또는 저급알이고 n은 1내지 10의 정수이며
    X 및 Y 중 적어도 하나가 시아노이면 다른 하나는 상기 유리의 카복시 또는 아미드화 또는 에스테르화 카복시 그룹이다.
  2. 제1항에 있어서, Ph는 비치환된 1,2-페닐렌 또는 저급알킬, 저급알콕시, 하이드록시 및 할로게노중에서 선택된 하나 또는 두개의 서로 같거나 다른 그룹으로 치환된 1,2-페닐렌 또는 저급알킬렌디옥시, 또는 트리플루오로 메틸중 한가지로 치환된 1,2-페닐렌이며 R0는 수소 또는 HPh이고 R1, R2및 R3는 각기 수소 또는 저급 알킬이고 n은 1내지 10의 정수인 일반삭(I)의 화합물 및 이의염을 제조하는 방법.
  3. 제1항에 있어서 Ph는 비치환 또는 저급알킬, 저급알콕시, 저급알킬렌디옥시, 하이드록시, 할로게노또는 트리플루오로 메틸등으로 1치환된 1,2-페닐렌이고 R0는 수소 또는 HPh이며 R1,R2및 R3는 각각 수소 또는 메틸이고 n은 2내지 8의 정수인 일반식(II)의 화합물 및 이들의 염이제조되는 방법.
  4. 제1항에 있어서, 다음 일반식(II)의 화합물 및 이들의 염이제조되는 방법.
    상기 일반식에서 R은 수소, 알킬 또는 탄소수 4이하의 알콕시, 할로게노 또는 트리플루오로 메틸이고
    m은 0 또는 1이며
    p와 q는 각각 0내지 2의 정수이고
    R1는 수소 또는 R-페닐이다.
  5. 제1항에 있어서, R은 수소, 메틸, 메톡시, 플루오로, 클로로 또는 트리플루오로메틸로서 바람직하게는 5-위치에 있으며 m과 p는 1이고 q는 1 또는 2이며 R1는 수소 또는 페닐인 일반식(II)의 화합물 및 이의 유도체가 제조되는 방법.
  6. 제1항에 있어서, 일반식(II)의 화합물이 2S-카복시-인돌린 평광성 에피머의 형태로 수득되는 방법.
  7. 제1항에 있어서, 1-(4-카보에톡시-2R,4R-디메틸부타노일)-인돌린 -2S-카복실산 또는 이들의 염이 제조되는 방법.
  8. 제1항에 있어서, 1-(4-카복시-2R,4R-디메틸부타노일)-인돌린-2S-카복실산 또는 이들의 염이 제조되는 방법.
  9. 제1항에 있어서, 1-(4-카보에톡시-2R-메틸-4R-펜에틸부타노일)-인돌린-2S-카복실산 또는 이들의 염이 제조되는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810004109A 1980-10-27 1981-10-27 1-카복시 알카노일 인돌린-2-카복실산 유도체의 제조방법 KR890000662B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US20070680A 1980-10-27 1980-10-27
US200.706 1980-10-27
US200,706? 1980-10-27
US06/235,294 US4374847A (en) 1980-10-27 1981-02-17 1-Carboxyalkanoylindoline-2-carboxylic acids
US235.294 1981-02-17

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KR830007551A true KR830007551A (ko) 1983-10-21
KR890000662B1 KR890000662B1 (ko) 1989-03-22

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US (1) US4374847A (ko)
EP (1) EP0050850B1 (ko)
KR (1) KR890000662B1 (ko)
AT (1) ATE26705T1 (ko)
AU (1) AU546726B2 (ko)
CA (1) CA1172257A (ko)
CY (1) CY1380A (ko)
DD (1) DD201887A5 (ko)
DE (1) DE3176125D1 (ko)
DK (1) DK154978C (ko)
ES (2) ES8303334A1 (ko)
FI (1) FI813349L (ko)
GB (1) GB2085880B (ko)
GR (1) GR74690B (ko)
HK (1) HK84687A (ko)
HU (1) HU185151B (ko)
IE (1) IE51688B1 (ko)
IL (1) IL64111A (ko)
MY (1) MY8700568A (ko)
NO (1) NO156979C (ko)
NZ (1) NZ198750A (ko)
PT (1) PT73879B (ko)

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DD201887A5 (de) 1983-08-17
DE3176125D1 (en) 1987-05-27
EP0050850A1 (de) 1982-05-05
ES506571A0 (es) 1983-02-01
MY8700568A (en) 1987-12-31
NO156979B (no) 1987-09-21
GR74690B (ko) 1984-07-03
IL64111A0 (ko) 1982-01-31
EP0050850B1 (de) 1987-04-22
ES8303334A1 (es) 1983-02-01
ES8401027A1 (es) 1983-12-01
AU7682381A (en) 1982-05-06
CA1172257A (en) 1984-08-07
ATE26705T1 (de) 1987-05-15
ES516561A0 (es) 1983-12-01
HU185151B (en) 1984-12-28
NZ198750A (en) 1984-05-31
GB2085880A (en) 1982-05-06
FI813349L (fi) 1982-04-28
HK84687A (en) 1987-11-20
NO156979C (no) 1987-12-30
IL64111A (en) 1984-10-31
DK154978C (da) 1989-06-12
PT73879A (de) 1981-11-01
KR890000662B1 (ko) 1989-03-22
US4374847A (en) 1983-02-22
NO813615L (no) 1982-04-28
CY1380A (en) 1987-08-07
AU546726B2 (en) 1985-09-19
DK470481A (da) 1982-04-28
DK154978B (da) 1989-01-16
IE51688B1 (en) 1987-02-04
GB2085880B (en) 1984-05-31
PT73879B (de) 1983-10-25

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