KR870001205A - 이속사졸 및 푸란의 제조방법 - Google Patents

이속사졸 및 푸란의 제조방법 Download PDF

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KR870001205A
KR870001205A KR1019860005307A KR860005307A KR870001205A KR 870001205 A KR870001205 A KR 870001205A KR 1019860005307 A KR1019860005307 A KR 1019860005307A KR 860005307 A KR860005307 A KR 860005307A KR 870001205 A KR870001205 A KR 870001205A
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compound
formula
alkyl
hydrogen
halogen
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KR1019860005307A
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KR900001314B1 (ko
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도미니크 다이애너 가이
도미니코 다이애너 가이
마이클 캐라바티즈 필립
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스터어링 드럭그 인코포레이팃드
벤자민 웃드로우 와이넛트
스터어링 드럭그 인코포이팃드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

내용 없음.

Description

이속사졸 및 푸란의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. a) 하기 구조식III)의 화합물을 산-수용체 존재하에 불활성 용매 중에서 가열하여 고리화해줌으로써 Y가 올레핀 결합이 개재된 알킬렌 다리를 나타내는 화합물들을 제외한, 옥사졸 또는 옥사진 고리의 4,5-위치에 이중 결합을 갖고 있지 않으며 R이 수소 또는 C1-3저급 알킬의 화합물을 제조하거나,
    (상기 식에서 Hal′은 염소 또는 브롬임) b) 하기 구조식(IV)의 화합물을 하기 구조식(V)의 화합물의 알칼리 금속염과 반응시켜 R1과 R2가 저급 알콕시 카보닐인 화합물을 제외한 X=O인 화합물을 얻은 다음
    (상기 식들에서 Hal은 염소, 브롬 또는 요드임) 소망에 따라; R이 하이드록시 알킬인 구조식(I)의 화합물을 산 할로겐화물 또는 산수물과 반응시켜 에스테르화하여 R이 저급-아실옥시인 화합물을 얻고; 소망에 따라; R이 하이드록시 알킬인 구조식(I)의 화합물을 강염기 존재하에 저급-알킬할로겐화물 또는 저급 알콕시 알킬 할로겐화물과 반응시켜 에테르화하여 R이 각기 저급-알콕시 또는 저급알콕시알콕시인 화합물을 얻고; 소망에 따라; 구조식(I)의 화합물을 지방족 하이드록시기를 할로겐으로 치환해 줄 수 있는 시약과 반응시켜 R이 할로겐에 의해 치환된 저급 알킬인 화합물을 얻고; 소망에 따라, R이 할로겐에 의해 치환된 저급 알킬인 화합물을 암모니아 또는 아민 NH=Z′와 반응시켜 N=Z1인 화합물을 제조하고; 소망에 따라, R이 아미노에 의해 치환된 저급알킬인 화합물을 저급-알카노일 할로겐화물 또는 무수물로 아실화하여 R이 저급 알카노일-아미노에 의해 치환된 알킬인 화합물을 얻고; 소망에 따라, 얻어진 염기 화합물을 그의 산부가염으로 전환시키는 것으로 구성된 하기 구조식(I)의 화합물의 제조 방법.
    상기 식에서 X는 O 또는 CH2이며; Y는 올레핀 결합이 임의로 개재된 C3-9알킬렌 다리이며, Z은 N 또는 R5C이며 R5는 수소 또는 저급알카노일이며, 단 Z이 N인 경우 R은 저급-알킬이며; m은 0 또는 1이며; R은 수소 또는 하이드록시, 저급-알콕시, 저급-알콕시알콕시, 저급-아실옥시, 할로, 또는 N=Z′에 의해 임의로 치환된 C1-3알킬이며 여기서 N=Z′는 아미노, 저급-알카노일아미노, 저급-알킬아미노, 디-저급알킬아미노, 1-피롤리딜, 1-피페리디닐, 4-모르폴리닐이며, R1및 R2는 할로겐, 메틸, 니트로, 저급-알콕시카보닐 또는 트리플루오로메틸이며; R3및 R4는 수소 또는 C1-3저급알킬이다.
  2. 제1항에 있어서, m이 0 또는 1이며, R이 메틸 또는 하이드록시메틸이며, R1과 R2가 각기 할로겐, 메틸, 니트로, 저급알콕시 카보닐 또는 트리플루오로메틸이며 R3과 R4가 각기 수소, 또는 C1-3저급 알킬인 하기 구조식의 화합물 또는 그의 제약상 허용되는 산-부가염을 제조하는 방법.
  3. 제2항에 있어서, 5-{5-[2,6-디클로로-4-(4,5-디하이드로-2-옥사졸릴)펜옥시]펜틸}-3-메틸이속사졸 또는 그의 제약상 허용되는 산부가염을 제조하는 방법.
  4. 하기 구조식(XII)의 화합물을 구조식의 화합물과 반응시키는 것으로 구성된 하기 구조식(III)의 화합물의 제조 방법.
    상기 식에서, X은 0 또는 CH2이며; Y는 C3-9알킬렌 다리이며; Z은 N 또는 R5C이며 여기서 R5는 수소 또는 저급알카노일이며; m은 0 또는 1이며; R1과 R2는 할로겐, 메틸, 니트로, 저급알콕시카보닐 또는 트리플루오로메틸이며; R, R3및 R4는 수소 또는 C1-3저급알킬이며 단 Z이 N인 경우 R은 저급알킬이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860005307A 1985-07-02 1986-07-01 신규한 이속사졸 및 푸란 KR900001314B1 (ko)

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US75134885A 1985-07-02 1985-07-02
US751.348 1985-07-02
US751348 1985-07-02

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KR900001314B1 KR900001314B1 (ko) 1990-03-08

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KR1019860005307A KR900001314B1 (ko) 1985-07-02 1986-07-01 신규한 이속사졸 및 푸란

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EP (2) EP0207453B1 (ko)
JP (2) JPH0819128B2 (ko)
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AR (4) AR241705A1 (ko)
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DE (3) DE3689924T4 (ko)
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GR (2) GR861695B (ko)
IE (2) IE66234B1 (ko)
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DE3689924T2 (de) 1995-01-19
NO862651L (no) 1987-01-05
AU5945786A (en) 1987-01-08
ZA864872B (en) 1987-02-25
ZA864873B (en) 1987-02-25
IL79309A (en) 1990-11-29
DK312986D0 (da) 1986-07-01
AU5945686A (en) 1987-01-08
AR242573A1 (es) 1993-04-30
FI862794A0 (fi) 1986-07-01
EP0207453A3 (en) 1988-11-23
NO862650D0 (no) 1986-07-01
KR900001315B1 (ko) 1990-03-08
ES8802517A1 (es) 1988-07-01
ES8802153A1 (es) 1988-04-01
NO165023B (no) 1990-09-03
GR861695B (en) 1986-11-04
KR870001202A (ko) 1987-03-12
NO165023C (no) 1990-12-12
EP0207454A3 (en) 1988-08-10
FI862795A (fi) 1987-01-03
IL79308A0 (en) 1986-10-31
EP0207453B1 (en) 1994-06-22
ES557779A0 (es) 1988-02-16
ATE107645T1 (de) 1994-07-15
JPH0768242B2 (ja) 1995-07-26
ATE80397T1 (de) 1992-09-15
MY102908A (en) 1993-03-31
DK173467B1 (da) 2000-12-04
FI862795A0 (fi) 1986-07-01
DK312986A (da) 1987-01-03
FI862794A (fi) 1987-01-03
ES8801649A1 (es) 1988-02-16
NO862651D0 (no) 1986-07-01
IE59755B1 (en) 1994-03-23
EP0207454B1 (en) 1992-09-09
EP0207453A2 (en) 1987-01-07
IL79309A0 (en) 1986-10-31
ES557778A0 (es) 1988-04-01
JPS6216480A (ja) 1987-01-24
FI85021B (fi) 1991-11-15
CA1280753C (en) 1991-02-26
AU587622B2 (en) 1989-08-24
NO164977C (no) 1990-12-05
ES8802518A1 (es) 1988-07-01
KR900001314B1 (ko) 1990-03-08
GR861697B (en) 1986-11-04
DE3686677T2 (de) 1993-03-11
NZ216678A (en) 1989-10-27
DE3689924D1 (de) 1994-07-28
DK171275B1 (da) 1996-08-19
PT82891A (en) 1986-08-01
PH23197A (en) 1989-05-29
PH22321A (en) 1988-07-29
IE66234B1 (en) 1995-12-13
NO862650L (no) 1987-01-05
NO164977B (no) 1990-08-27
PT82892B (pt) 1994-09-30
CA1299176C (en) 1992-04-21
AU589190B2 (en) 1989-10-05
IE861724L (en) 1987-01-02
DE3686677D1 (de) 1992-10-15
AR242572A1 (es) 1993-04-30
MX2954A (es) 1993-11-01
FI85021C (fi) 1992-02-25
MX9100032A (es) 1993-01-01
DK313086A (da) 1987-01-03
PT82892A (pt) 1987-01-26
ES557780A0 (es) 1988-02-16
ES556811A0 (es) 1988-07-01
PT82891B (pt) 1988-05-27
EP0207454A2 (en) 1987-01-07
ES556812A0 (es) 1988-07-01
DK313086D0 (da) 1986-07-01
MX9100029A (es) 1993-01-01
AR244686A1 (es) 1993-11-30
JPS6216479A (ja) 1987-01-24
ES8801651A1 (es) 1988-02-16
IE861723L (en) 1987-01-02
AR241705A1 (es) 1992-11-30
MX9100033A (es) 1993-01-01
DE3689924T4 (de) 1995-05-11
JPH0819128B2 (ja) 1996-02-28
IL79308A (en) 1991-01-31

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