KR890005083A - 항균제로서 유용한 4-옥소-3-퀴놀린카르복실산 및 그 제조방법 - Google Patents

항균제로서 유용한 4-옥소-3-퀴놀린카르복실산 및 그 제조방법 Download PDF

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Publication number
KR890005083A
KR890005083A KR1019880011552A KR880011552A KR890005083A KR 890005083 A KR890005083 A KR 890005083A KR 1019880011552 A KR1019880011552 A KR 1019880011552A KR 880011552 A KR880011552 A KR 880011552A KR 890005083 A KR890005083 A KR 890005083A
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South Korea
Prior art keywords
hydrogen
compound
fluoro
pyridinyl
cyclopropyl
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KR1019880011552A
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English (en)
Inventor
요오 레셔 조오지
사인 발디브
류우먼 마이클
Original Assignee
폴 에밀 듀폰드
스터어링 드럭그 인코포레이팃드
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Application filed by 폴 에밀 듀폰드, 스터어링 드럭그 인코포레이팃드 filed Critical 폴 에밀 듀폰드
Publication of KR890005083A publication Critical patent/KR890005083A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46—Friedel-Crafts reactions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/80—Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • C07C49/807—Ketones containing a keto group bound to a six-membered aromatic ring containing halogen all halogen atoms bound to the ring
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond

Abstract

내용 없음

Description

항균제로서 유용한 4-옥소-3-퀴놀린카르복실산 및 그 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (9)

  1. 하기 일반식을 갖는 화합물 또는 제약학적으로 허용 가능한 그의 산-부가염; 또는 R이 수소인 화합물의 알카리 금속 또는 아민염 :
    상기식에서, R은 수소 또는 저급-알킬이고 ; R' 수소, 플루오로 또는 -SR″'이고, R'″는 페닐, 벤질 또는 저급-알킬이고 ; R″는 수소, 플루오로 및 -SR″'로부터 선택되는데, 단 R"이 수소인 경우, R' 또한 수소이다.
  2. 제1항에 있어서, R이 수소이고 R' 및 R″가 수소 또는 플루오로인 화합물.
  3. 제2항에 있어서, 1-시클로프로필-7-(2,6-디메틸-4-피리디닐)-5,6,8-트리플루오로-1,4-디히드로-4-옥소-3-퀴놀린카르복실산.
  4. 제2항에 따른1-시클로프로필-7-(2,6-디메틸-4-피리디닐)-6-플루오로-1,4-디히드로-4-옥소-3-퀴놀린카르복실산.
  5. 제2항에 따른1-시클로로프로필-6,8-디플루오로-1,4-디히드로-7-(2,6-디메틸-4-피리디닐)-4-옥소-3-퀴놀린카르복실산.
  6. 제1항에 따른 1-시클로프로필-7-(2,6-디메틸-4-피리디닐)-6-플루오로-1,4-디히드로-5-(페닐티오)-3-퀴놀린카르복실산.
  7. 제1항에 따른,1-시클로프로필-7-(2,6-디메틸-4-피리디닐)-6-플루오로-1,4-디히드로-8-(벤질티오)-3-퀴놀린카르복실산.
  8. R이 저급-알킬이고, 각 R' 및 R″가 수소 또는 플루오로이고 X가 염소, 브롬 또는 요오드인 다음 일반식의 화합물 ;
    을 Alk가 1-6개의 탄소원자를 갖는 알킬인 다음 일반식의 화합물 ;
    과 반응시켜 일반식I의 상응 화합물을 제조하고 ; 원한다면, 얻어진 일반식 I의 화합물을 가수분해시켜 R이 수소인 상응 화합물을 얻고, 원한다면, R'이 플루오로인 일반식 I의 화합물을 황화물, R″'SH와 반응시켜 R'가-SR″'인 일반식 I의 화합물을 생성시키고, 원한다면, 이 화합물을 라네이 리켈과 함께 가열시켜 -SR″'기를 수소로 치환시키고; 원한다면, 얻어진 유리 염기를 전환시켜 그 산 부가염을 얻고, 원하다면, R이 수소인 얻어진 화합물을 염기와 반응시켜 그 알카리 금속 또는 아민 염을 얻는 것으로 이루어진 제1항 또는 제2항에 따른 화합물을 제조하는 방법.
  9. 항균적 유효량의 제1항에 따른 화합물과 하나 또는 그 이상의 제약학적으로 허용 가능한 부형제, 희석제, 담체 또는 용매를 포함하는 세균 방제용 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019880011552A 1987-09-08 1988-09-07 항균제로서 유용한 4-옥소-3-퀴놀린카르복실산 및 그 제조방법 KR890005083A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9435987A 1987-09-08 1987-09-08
US094,359 1987-09-08

Publications (1)

Publication Number Publication Date
KR890005083A true KR890005083A (ko) 1989-05-11

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KR1019880011552A KR890005083A (ko) 1987-09-08 1988-09-07 항균제로서 유용한 4-옥소-3-퀴놀린카르복실산 및 그 제조방법

Country Status (15)

Country Link
EP (1) EP0309789A1 (ko)
JP (1) JPH01100166A (ko)
KR (1) KR890005083A (ko)
AR (1) AR247553A1 (ko)
AU (1) AU598394B2 (ko)
DK (1) DK493988A (ko)
FI (1) FI884106A (ko)
IL (1) IL87569A (ko)
MX (1) MX12881A (ko)
MY (1) MY103910A (ko)
NO (1) NO170930C (ko)
NZ (1) NZ225926A (ko)
PH (1) PH26759A (ko)
PT (1) PT88431B (ko)
ZA (1) ZA886400B (ko)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5169853A (en) * 1987-09-08 1992-12-08 Sterling Drug Inc. Pyridinyl-quinolone compounds, their preparation and use
US5075319A (en) * 1987-09-08 1991-12-24 Sterling Drug Inc. Pyridinyl-quinolone compounds, their preparation and use
US4996355A (en) * 1989-04-14 1991-02-26 Mallinckrodt, Inc. Novel intermediates for the production of 2,4,5-trifluorobenzoyl fluoride
KR100204987B1 (ko) 1990-04-18 1999-06-15 제이코버스 코넬리스 레이서 항미생물성 퀴놀로닐 락탐
CN1338455A (zh) * 2000-08-16 2002-03-06 大连绿源实业有限公司 新的喹诺酮羧酸的制备方法
WO2010058421A2 (en) * 2008-11-18 2010-05-27 Aditya Birla Science & Technology Co. Ltd. A process for synthesis of 2, 4-dichloro-5- fluoroacetophenone (dcfa)
CN107686456B (zh) * 2017-07-25 2018-10-23 杭州师范大学 一种喹喏酮关键中间体乙酯胺化物及其制备方法和应用

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3907808A (en) * 1971-05-17 1975-09-23 Sterling Drug Inc 1,4-Dihydro-4-oxo-7-pyridyl-3-quinolinecarboxylic acid derivatives
US3753993A (en) * 1971-05-17 1973-08-21 Sterling Drug Inc 1,4-dihydro-4-oxo-7-pyridyl-3-quinoline-carboxylic acid derivatives
US4670444B1 (en) * 1980-09-03 1999-02-09 Bayer Ag and-naphthyridine-3-carboxylic acids and antibacte7-amino-1-cyclopropyl-4-oxo-1,4-dihydro-quinoline-rial agents containing these compounds
NZ208470A (en) * 1983-07-18 1988-06-30 Abbott Lab 6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid derivatives and antibacterial compositions containing such
US4529725A (en) * 1984-04-26 1985-07-16 Abbott Laboratories 1-Pyridine substituted quino-benzothiazine
EP0179239A3 (en) * 1984-09-17 1986-08-13 Sterling Drug Inc. 7-(pyridinyl)-/-alkyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid having antibacterial activity and preparation thereof
US4636506A (en) * 1984-12-06 1987-01-13 Pfizer, Inc. 7-heterocyclic-1,4-dihydroquinolones

Also Published As

Publication number Publication date
IL87569A0 (en) 1989-01-31
PT88431A (pt) 1989-07-31
PT88431B (pt) 1992-10-30
MY103910A (en) 1993-10-30
NO883897L (no) 1989-03-09
DK493988D0 (da) 1988-09-06
AU598394B2 (en) 1990-06-21
IL87569A (en) 1992-08-18
NO170930B (no) 1992-09-21
ZA886400B (en) 1989-04-26
AU2184388A (en) 1989-03-09
NO883897D0 (no) 1988-09-01
PH26759A (en) 1992-09-28
MX12881A (es) 1993-08-01
EP0309789A1 (en) 1989-04-05
DK493988A (da) 1989-03-09
FI884106A (fi) 1989-03-09
AR247553A1 (es) 1995-01-31
NO170930C (no) 1992-12-30
NZ225926A (en) 1990-04-26
FI884106A0 (fi) 1988-09-06
JPH01100166A (ja) 1989-04-18

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