KR840005816A - 세팜로스포틴 화합물의 제조방법 - Google Patents

세팜로스포틴 화합물의 제조방법 Download PDF

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KR840005816A
KR840005816A KR1019830003647A KR830003647A KR840005816A KR 840005816 A KR840005816 A KR 840005816A KR 1019830003647 A KR1019830003647 A KR 1019830003647A KR 830003647 A KR830003647 A KR 830003647A KR 840005816 A KR840005816 A KR 840005816A
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salt
compound
medicament
hydrogen
general formula
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KR1019830003647A
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KR870001440B1 (ko
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도요나리(외 4) 오오이네
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마쓰바라 이찌로오
다나베 세이야구 가부시기가이샤
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/247-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • C07D501/26Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group
    • C07D501/34Methylene radicals, substituted by oxygen atoms; Lactones thereof with the 2-carboxyl group with the 7-amino radical acylated by carboxylic acids containing hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D501/00Heterocyclic compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D501/14Compounds having a nitrogen atom directly attached in position 7
    • C07D501/16Compounds having a nitrogen atom directly attached in position 7 with a double bond between positions 2 and 3
    • C07D501/207-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids
    • C07D501/247-Acylaminocephalosporanic or substituted 7-acylaminocephalosporanic acids in which the acyl radicals are derived from carboxylic acids with hydrocarbon radicals, substituted by hetero atoms or hetero rings, attached in position 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

내용 없음

Description

세팜로스포틴 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (35)

  1. (ⅰ) 일반식 :
  2. 의 화합물 또는 이것의 반응유도체를 일반식 :
  3. 의 화합물 또는 이것의 염으로 축합시키는 것;
  4. (ⅱ) 그 보호기 또 기들을 제거하는 것; 및
  5. (ⅲ) 만일 필요하다면 전술한 생성물을 이것의 약제로 사용할 수 있는 염으로 전환시키는 공정을 포함하는 것으로 된 일반식 :
  6. 의 7β-〔(Z)-2-(2-아마노티아졸-4-일)-2-옥시아마노-아세트아마도〕-3-세펨-4-카르복시산 화합물 또는 이것의 약제로 사용할 수 있는 염의 제조방법.
  7. (위 식에서, R1은 수소 또는 저급알킬이고; R2는 아세톡시 또는 (1-메틸-1H-테트라졸-5-일)리오이며, R3는 카르복시이거나; 또는 R2는 일반식 :의 기이며, R3는 -COO-이고, Y는 수소, 히드록시메틸 또는 카르바모일이고; 그리고 n은 2 또는 3의 정수이다. 또한 R4는 보호기이고; R5는 R2가 아세톡시 또는(1-메틸-1H-테트라졸-5-일) 티오일 때에는 보호 카르복시이고, R2가 일반식:의 기 일때에는 -CCO-이다.)
  8. 일반식 :
  9. (ⅰ)
  10. 의 화합물 또는 이것의 염을 일반식 :
  11. 의 피리딘 화합물, (1-페닐-5-페르캅토) 테트라졸 또는 이것의 염과 반응시키는 것;
  12. (ⅱ) R7이 보호기인 경우에는 동일 보호기를 제거하는 것; 및
  13. (ⅲ) 만일 필요하다면 전술한 생성물을 이것의 약제로 사용할 수 있는 염으로 전환시키는 공정으로 된 일반식:
  14. 의 7β-〔(Z)-2-(2-아마노티아졸-4-일)-2-옥시아마노-아세트아마도〕-3-세펨-4-카르복시산 화합물 또는 이것의 약제로 사용할 수 있는 염의 제조방법.
  15. 위 식에서, R1은 수소 또는 저급알킬이고; R6은 (1-메틸-1H-테트라졸-5-일)티오, 그리고 R3는 카르복시이거나; 또는 R6이 일반식 :의 기, R3이 -COO-이고, 그리고 Y가 수소, 히드록시메틸 또는 카르바모일; 그리고 n이 2 또는 3의 정수이며 R7은 수소 또는 보호기이고, 또 Y와 n은 앞에서 정의한 바와 같다.
  16. 항마생물 유효량의 일반식 :
  17. 의 7β-〔(Z)-2-(2-아마노티아졸-4-일)-2-옥시아마노-아세트아마도〕-3-세펨-4-카르복시산 화합물 또는 이것의 약제로 사용할 수 있는 염과 약제로 사용할 수 있는 캐리어를 함유하는 약제조성물.
  18. 위 식에서, R1,R2,R3, Y 및 n은 앞에서 정의한 바와 같다.
  19. 제3항에서 전술한 세팔로스포틴 화합물이 R1이 수소, R2가 일반식 :의 기, R3가 -COO-Y가 수소, 4-히드록시메틸, 3-히드록시메틸 또는 4-카르바모일 그리고 n이 2의 정수인 일반식(Ⅰ)의 화합물인 약제 조성물.
  20. 제3항에서 전술한 세팔로스포린 화합물이 7β-{(Z)-2-(2-아미노티아졸-4-일) -2-〔2-피르롤리든-3-일)옥시이미노〕아세트아미}도-3-(1-피리디니오메틸)-3-세펨-4-카르복실레이트 또는 이것의 약제로 사용할 수 있는 염인 약제 조성물.
  21. 제3항에서 전술한 세팔로스포린 화합물이 7β-{(Z)-2-(2-아미노티아졸-4-일) -2-〔(3S)-2-피르롤리든-3-일)옥시이미노〕-아세트아미도}-3-(1-피리디니오메틸)-3-세펨-4-카르복실레이트 또는 이것의 약제로 사용할 수 있는 염인 약제조성물.
  22. 온혈동물에 항미생물 유효량의 일반식 :
  23. 의 7β-〔(Z)-2-(2-아마노티아졸-4-일)-2-옥시아마노-아세트아마도〕-3-세펨-4-카르복시산 화합물 또는 이것의 약제로 사용할 수 있는 염을 투약하는 것으로 된 미생물 전염병 치료방법, 위 식에서 R1,R2,R3, Y 및 n은 앞에서 정의한 바와 같다.
  24. 제7항에서 전술한 세팔로스포린 화합물이, R1이 수소, R2가 일반식 :의 기, R3가 -COO-Y가 수소, 4-히드록시메틸, 3-히드록시메틸 또는 4-카르바모일 그리고 n이 2의 정수인 방법.
  25. 제7항에서 진술한 세팔로스포린 화합물이 7β-{(Z)-2-(2-아미노티아졸-4-일) -2-〔2-피르롤리든-3-일)옥시이미노〕-아세트아미도}-3-(1-피리디니오메틸)-3-세펨-4-카르복실레이트 또는 이것의 약제로 사용할 수 있는 염인방법.
  26. 제7항에서 전술한 세팜로스포린 화합물이 7β-{(Z)-2-(2-아미노티아졸-4-일) -2-〔(3S)-2-피르롤리든-3-일)옥시이미노〕-아세트아미도}-3-(1-피리디니오메틸)-3--4-세펨카르복실레이트 또는 이것의 약제로 사용할 수 있는 염인방법.
  27. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019830003647A 1982-08-07 1983-08-04 세팔로스포린 화합물의 제조방법 KR870001440B1 (ko)

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KR1019870005206A KR870001441B1 (ko) 1982-08-07 1987-05-26 세팔로스포린 화합물의 제조방법

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GB82-22823 1982-08-07
GB8222823 1982-08-07
JP22823 1982-08-07

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US (4) US4598075A (ko)
EP (2) EP0101265B1 (ko)
JP (3) JPS5951292A (ko)
KR (1) KR870001440B1 (ko)
AT (2) ATE35413T1 (ko)
AU (1) AU562248B2 (ko)
BG (3) BG40967A3 (ko)
CA (1) CA1231940A (ko)
CS (2) CS243484B2 (ko)
DD (1) DD210053A5 (ko)
DE (2) DE3381734D1 (ko)
DK (2) DK358983A (ko)
ES (3) ES8502121A1 (ko)
FI (1) FI74972C (ko)
GR (1) GR78864B (ko)
IE (1) IE55406B1 (ko)
IL (1) IL69246A (ko)
NO (1) NO161068C (ko)
PH (1) PH18498A (ko)
PL (2) PL139932B1 (ko)
PT (1) PT77166B (ko)
SU (2) SU1227116A3 (ko)
ZA (1) ZA835411B (ko)

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JPS6185392A (ja) * 1984-10-03 1986-04-30 Tanabe Seiyaku Co Ltd セフアロスポリン化合物の新規製法
JPS61143381A (ja) * 1984-12-14 1986-07-01 Tanabe Seiyaku Co Ltd 光学活性チアゾ−ル酢酸誘導体の製法
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JPS61171464A (ja) * 1985-01-23 1986-08-02 Dai Ichi Seiyaku Co Ltd オキシイミノ酪酸誘導体の製法
JPS63107989A (ja) * 1986-06-04 1988-05-12 Tanabe Seiyaku Co Ltd セファロスポリン化合物
IL82738A0 (en) * 1986-06-16 1987-12-20 Tanabe Seiyaku Co Cephalosporin compounds,their preparation and pharmaceutical compositions containing them
AT389701B (de) * 1987-10-08 1990-01-25 Tanabe Seiyaku Co Neue cephalosporinverbindungen und diese enthaltende pharmazeutische zusammensetzungen
JP4773154B2 (ja) * 2005-07-29 2011-09-14 小澤物産株式会社 レバー式カップリング

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GB1399086A (en) * 1971-05-14 1975-06-25 Glaxo Lab Ltd Cephalosporin compounds
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IE55406B1 (en) 1990-09-12
AU562248B2 (en) 1987-06-04
JPH0246588B2 (ko) 1990-10-16
BG40967A3 (en) 1987-03-14
DK361587D0 (da) 1987-07-10
CS243484B2 (en) 1986-06-12
ATE54450T1 (de) 1990-07-15
KR870001440B1 (ko) 1987-08-06
ES531296A0 (es) 1985-08-01
FI74972B (fi) 1987-12-31
NO161068C (no) 1989-06-28
FI74972C (fi) 1988-04-11
ES8603496A1 (es) 1985-12-16
IE831648L (en) 1984-02-07
JPS62294681A (ja) 1987-12-22
EP0245619B1 (en) 1990-07-11
CS196483A2 (en) 1985-08-22
PL139932B1 (en) 1987-03-31
US4742174A (en) 1988-05-03
JPH0145473B2 (ko) 1989-10-03
EP0101265B1 (en) 1988-06-29
DK358983A (da) 1984-02-08
NO161068B (no) 1989-03-20
DE3377213D1 (en) 1988-08-04
FI832770A0 (fi) 1983-08-02
US4598075A (en) 1986-07-01
ES535281A0 (es) 1985-12-16
BG37838A3 (en) 1985-08-15
NO832828L (no) 1984-02-08
ES524775A0 (es) 1984-12-16
DK361587A (da) 1987-07-10
EP0101265A3 (en) 1985-04-10
ATE35413T1 (de) 1988-07-15
ES8506707A1 (es) 1985-08-01
PL243329A1 (en) 1985-02-13
US4598154A (en) 1986-07-01
BG42835A3 (en) 1988-02-15
GR78864B (ko) 1984-10-02
PT77166A (en) 1983-09-01
PT77166B (pt) 1986-01-28
SU1227116A3 (ru) 1986-04-23
DE3381734D1 (de) 1990-08-16
JPS62294615A (ja) 1987-12-22
JPS5951292A (ja) 1984-03-24
IL69246A (en) 1986-07-31
ES8502121A1 (es) 1984-12-16
EP0101265A2 (en) 1984-02-22
CS236798B2 (en) 1985-05-15
ZA835411B (en) 1984-03-28
PL249964A1 (en) 1985-05-07
PH18498A (en) 1985-08-02
PL140023B1 (en) 1987-03-31
JPH0360803B2 (ko) 1991-09-17
IL69246A0 (en) 1983-11-30
AU1710483A (en) 1984-02-09
SU1324586A3 (ru) 1987-07-15
CA1231940A (en) 1988-01-26
FI832770A (fi) 1984-02-08
EP0245619A1 (en) 1987-11-19
US4727071A (en) 1988-02-23
DK358983D0 (da) 1983-08-05
DD210053A5 (de) 1984-05-30

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