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KR860007280A - 카르바사이클린 유도체의 제조방법 - Google Patents

카르바사이클린 유도체의 제조방법 Download PDF

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Publication number
KR860007280A
KR860007280A KR1019860002033A KR860002033A KR860007280A KR 860007280 A KR860007280 A KR 860007280A KR 1019860002033 A KR1019860002033 A KR 1019860002033A KR 860002033 A KR860002033 A KR 860002033A KR 860007280 A KR860007280 A KR 860007280A
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South Korea
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group
compound
represent
general formula
methyl
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KR890003841B1 (ko
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고이찌 고지마
신사꾸 고바야시
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상꾜 가부시끼가이샤
가와무라 요시부미
상꾜 가부시끼 가이샤
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • C07C405/005—Analogues or derivatives having the five membered ring replaced by other rings
    • C07C405/0075—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system
    • C07C405/0083—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system which is only ortho or peri condensed, e.g. carbacyclins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C13/00—Cyclic hydrocarbons containing rings other than, or in addition to, six-membered aromatic rings
    • C07C13/28—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof
    • C07C13/32—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings
    • C07C13/36—Polycyclic hydrocarbons or acyclic hydrocarbon derivatives thereof with condensed rings with a bicyclo ring system containing five carbon atoms
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

카르바사이클린 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 하기 일반식(Ⅴ)의 화합물로부터 히드록시-보호기 R4및 R5를 제거하여 하기 일반식(Ⅰ)의 화합물을 수득하고, 임의로 일반식(Ⅰ)의 화합물을 염화시켜 그의 약학적으로 허용되는 염을 수득함을 특징으로 하는 하기 일반식(Ⅰ)을 갖는 카르바사이클린 유도체 또는 약학적으로 허용되는 그의 염을 제조하는 방법.
    (Ⅴ)
    (상기 식중,
    R1은 수소원자 또는 1∼10탄소 원자의 알킬기로 구성된 군으로 부터 선택된 기이고,
    R2는 수소원자 및 메틸기로 구성된 군으로 부터 선택된 기이고,
    R3은 부테닐기, 4-펜테닐기 또는 5-메틸-4-헥세닐기이고,
    R4및 R5는 같거나 다르며, 각각 히드록시-보호기를 나타낸다.)
  2. 제 1 항에 있어서, R1이 수소원자 또는 메틸기임을 특징으로 하는 방법.
  3. 제 1 항 또는 2항에 있어서, R2가 메틸기임을 특징으로 하는 방법.
  4. 제 3 항에 있어서, R3이 3-부테닐기 또는 4-펜테닐기임을 특징으로 하는 방법.
  5. 제 4 항에 있어서, R3이 4-펜테닐기임을 특징으로 하는 방법.
  6. 제 1 항에 있어서, 일반식(Ⅰ)의 화합물이 하기 일반식(Ⅰa)로 나타내지는 입체화학을 가짐을 특징으로 하는 방법.
    (상기식중, R1,R2및 R3은 상기 정의와 동일하다.)
  7. 제 1 항에 있어서, 카르바사이클린 유도체가 16,16-디메틸-19,20-디데히드로카르바사이클린 및 약학적으로 허용되는 그의 염, 16-메틸-20-메틸렌카르바사이클린 및 약학적으로 허용되는 그의 염, 16,16-디메틸-20-메틸렌카르바사이클린 및 약학적으로 허용되는 그의 염 및 16,16-디메틸-20-메틸렌카르바사이클린 메틸 에스테르임을 특징으로 하는 방법,
  8. 제 1 항에 있어서, R4및 R5가 각각 헤테로사이클기를 나타냄을 특징으로 하는 방법.
  9. 제 8 항에 있어서, R4및 R5가 각각 테트라히드로 피라닐 또는 4-메톡시테트라히드로피란-4-일기를 나타냄을 특징으로 하는 방법.
  10. 제 8 항에 있어서, R4및 R5가 각각 치환된 메틸기를 나타냄을 특징으로 하는 방법.
  11. 제 8 항에 있어서, R4및 R5가 각각 매톡시메틸 또는 벤질옥시메틸기를 나타냄을 특징으로 하는 방법.
  12. 제 8 항 내지 11항중 어느 하나에 있어서, 일반식(Ⅴ)의 화합물을 불활성용매내에서 산으로 처리함으로써 보호기 R4및 R5를 제거함을 특징으로 하는 방법.
  13. 제 12 항에 있어서, 실온 ∼100℃에서 30분∼5시간에 걸쳐 보호기 R4및 R5를 제거함을 특징으로 하는 방법.
  14. 제 8 항에 있어서, R4및 R5가 각각 실릴기를 나타냄을 특징으로 하는 방법.
  15. 제 14 항에 있어서, R4및 R5가 각각 디메틸-t-부틸실릴기를 나타냄을 특징으로 하는 방법.
  16. 제14항 또는 15항에 있어서, 화합물(Ⅴ)을 물안에서 산, 염기 또는 테트라부염암모늄 플루오라이드로 처리하거나 또는 불활성용매내에서 암모늄염으로 처리하여 보호기 R4및 R5를 제거함을 특징으로 하는 방법.
  17. 제16항에 있어서, 화합물(Ⅴ)을 물안, 실온근처에서 30분∼3시간동안 산, 염기 또는 테트라부틸암모늄 플루오라이드로 처리함으로써 보호기 R4및 R5를 제거함을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860002033A 1985-03-19 1986-03-19 카르바사이클린 유도체의 제조방법 Expired KR890003841B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP55305 1985-03-19
JP5530585 1985-03-19
JP60-55305 1985-03-19

Publications (2)

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KR860007280A true KR860007280A (ko) 1986-10-10
KR890003841B1 KR890003841B1 (ko) 1989-10-05

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KR1019860002033A Expired KR890003841B1 (ko) 1985-03-19 1986-03-19 카르바사이클린 유도체의 제조방법

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US (1) US4757087A (ko)
EP (1) EP0195668B1 (ko)
JP (1) JPS6216A (ko)
KR (1) KR890003841B1 (ko)
AT (1) ATE63537T1 (ko)
CA (1) CA1251202A (ko)
DE (1) DE3679224D1 (ko)
ES (1) ES8707489A1 (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4576102A (en) * 1983-09-02 1986-03-18 Waste-Tech Services, Inc. Removal of tramp material from fluid bed vessels
US4553487A (en) * 1983-09-02 1985-11-19 Waste-Tech Services, Inc. Removal of tramp material from fluid bed vessels
DE3608088C2 (de) * 1986-03-07 1995-11-16 Schering Ag Pharmazeutische Präparate, enthaltend Cyclodextrinclathrate von Carbacyclinderivaten

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5495552A (en) * 1978-01-06 1979-07-28 Sankyo Co Ltd Prostacyline derivative and its preparation
GB2038333B (en) * 1978-01-26 1982-10-06 Erba Farmitalia 12 -formyl- (20 12)octanor-9-deoxy-9 -methylene pgi derivatives
US4238414A (en) * 1978-02-13 1980-12-09 The Upjohn Company 2-Decarboxy-2-aminomethyl-6a-carba-PGI2 compounds
DE2845770A1 (de) * 1978-10-19 1980-04-30 Schering Ag Neue prostacyclin-derivate und verfahren zu ihrer herstellung
US4338457A (en) * 1980-02-28 1982-07-06 The Upjohn Company Composition and process
US4628110A (en) * 1982-02-16 1986-12-09 The Upjohn Company Novel 9-substituted carbacyclin analogs

Also Published As

Publication number Publication date
KR890003841B1 (ko) 1989-10-05
ATE63537T1 (de) 1991-06-15
ES553166A0 (es) 1987-08-01
CA1251202A (en) 1989-03-14
EP0195668A2 (en) 1986-09-24
DE3679224D1 (de) 1991-06-20
EP0195668A3 (en) 1987-09-30
JPH0584295B2 (ko) 1993-12-01
EP0195668B1 (en) 1991-05-15
ES8707489A1 (es) 1987-08-01
JPS6216A (ja) 1987-01-06
US4757087A (en) 1988-07-12

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