KR830009138A - 스테로이드의 방향성 헤테로사이클릭 에스테르와 이들의 제법 및 이들을 함유하는 약제학적 조성물 - Google Patents

스테로이드의 방향성 헤테로사이클릭 에스테르와 이들의 제법 및 이들을 함유하는 약제학적 조성물 Download PDF

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KR830009138A
KR830009138A KR1019820000374A KR820000374A KR830009138A KR 830009138 A KR830009138 A KR 830009138A KR 1019820000374 A KR1019820000374 A KR 1019820000374A KR 820000374 A KR820000374 A KR 820000374A KR 830009138 A KR830009138 A KR 830009138A
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hydrogen
fluorine
methyl
chlorine
formula
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KR1019820000374A
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KR890000761B1 (ko
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엘. 사피로 엘리오트
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스테이나 칸스타드,로즈마리 아이젠링
쉐링 코포레이션
로즈마리 아이젠링
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)

Abstract

내용 없음

Description

스테로이드의 방향성 헤테로사이클릭 에스테르와 이들의 제법 및 이들을 함유하는 약제학적 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (8)

  1. 하기 A, B, C, D 방법중의 하나 또는 하나 이상의 방법으로 구성된 방법을 특징으로 하여 일반식(I)의 3,20-디옥소-1,4-프레그나디엔-17α-올 17방향족 헤테로사이클릭 카복실레이트를 제조하는 방법.
    A) 일반식(I)에 상응하는 출발물질의 16α,17α 및/또는 21위치중의 하나 이상의 위치에 목적하는 에스테르화 그룹을 도입시킨다.
    B) 일반식(I)에 상응하는 출발물질의 11β,16α 및 21위에 존재하는 에스테르중의 하나 이상을 가수분해시킨다.
    C) 9(11)-엔, 9β,11β-에폭사이드 또는 21-활성 아실레이트 출발물질의 9α,11β 및 21위치중의 하나 또는 그 이상 위치를 할로겐화시켜 일반식(I)의 상응하는 9β,11β-디할로, 9α-할로-11β-하이드록시 또는 21-할로-화합물을 제조한다.
    D) 11-은 출발물질의 11-케토그룹을 환원시켜 일반식(I)의 상응하는 11β-하이드록시 화합물을 제조한다.
    상기식에서
    A는 수소이거나, 또는 Y가(H, βOH)일 때는 A는 염소, 불소 또는 메틸일 수있으며,
    X는 수소 또는 원자량 100이하의 할로겐원자이고;
    Y는 산소, (H,βOH)이거나, 또는 X가 염소, 브롬일 때 Y는(H,β-할로겐), 원자량이 100이하이고 적어도 X와 동일한 전기음성도를 지니는 β-할로겐이며;
    Z는 수소, 메틸, 염소 또는 불소이고;
    Z'는 수소이거나 또는 Z가 수소일때는 원자량 100이하의 할로겐이고;
    V는 티오펜카복실산, 피롤카복실산, 또는 푸란카복실산의 아실그룹 또는 이들의 메틸 또는 할로겐-치환된 유도체이며;
    W는 (H,H), (H, 저급알킬, (H, αOV1)(여기서 V1은 수소 또는 레티노산 또는 탄소수 12까지의 카복실산의 아실기이다) 또는 =CHT(여기서 T는 수소, 저급알킬, 불소 또는 염소이다)이며;
    G는 수소, 분자량 100이하의 할로겐원자 또는 -QV2(여기서 Q는 산소 또는 유황원자이고 V2는 V 또는 V1에서 정의된 바와 같거나 또는 인산의 아실기이며 이 인산은 모노- 또는 디-알칼리금속염 또는 알칼리토금속염의 형태로 존재할 수 있다)이다.
  2. A 및 Z'가 모두 수소이고 X와 Y가 모두 염소이고 또는 X는 α-불소이고 Y는 β-하이드록시이고, Z는 수소 또는 불소이고 W는 메틸 특히 α-메틸이고, G는 상기 -QV2에서 정의된 아실기인 일반식(I)에 상응하는 3,20-디옥소-1,4-프레그나디엔 17α,21-디올 21-아실레이트를 푸란 또는 티오펜카복실산의 활성 유도체로 에스테르화 시킴을 특징으로 하는 상기 1의 제법 A에 따른 방법.
  3. A와 Z'이 모두 수소이고, X와 Y는 일반식(I)에서 정의된 바와 같고 Z는 수소 또는 불소이고 W는 메틸, 특히 α-메틸인 일반식(I) 상응하는 17α-푸로에이트-21-아실레이트 또는 17α-테노에이트-21-아실레이트 또는 17α,21-오르토 에스테르 즉, 17α,21-알킬 오르토-푸로에이트 또는 레노에이트의 21위치를 가수분해시켜 수득된 17α,21-디올 17α-푸로에이트 또는 테노에이트의 21위치를 재에스테르화시켜 다른 목적하는 일반식(I)의17α,21-디에스테르를 제조함을 특징으로 하는 상기 1의 제법 B에 따른 방법.
  4. A와 Z'가 모두 수소이고 X는 α-불소이고 Y는 β-하이드록시이고 Z는 수소 또는 불소이고 W는 메틸 특히 α-메틸이고 V는 푸란- 또는 티오펜-카복실산의 아실잔기인 일반식(I)에 상응하는 3,20-디옥소-1,4-프레그니디엔 21-활성 아실레이트, 예를 들어 21-설포네이트의 21 위치를 적합한 염소이온 공급원으로 염소화시킴을 특징으로 하는 상기 1의 제법 C에 따른 방법.
  5. A와 Z'가 모두 수소이고, Z는 수소 또는 불소 W는 메틸, 특히 α-메틸이고 G는 염소, 불소 또는 상기 -QV2에서 정의된 아실기이고, V는 푸란- 또는 티오펜-카복실산의 아실기인 일반식(I)에 상용하는 3,20-디옥소-1,4,9(11)-프레그나트리엔의 9(11)-이중결합내에 염소 또는 9α-염소 및 11β-하이드록시 그룹을 부가 반응시켜 각각의 일반식(I)의 9α,11β-디클로로- 및 9α-클로로-11β-하이드록시 화합물을 얻고 다시 21-아실레이트를 상용하는 21-클로로기로 전환시킴을 특징으로 하는 상기 1의 제법 C에 따른 방법.
  6. A와 Z'가 모두 수소이고 Z는 수소 또는 불소이고 W는 메틸 특히 α-메틸이고 G는 염소, 불소 또는 상기 -QV2에서 정의된 아실기이고 V는 푸란- 또는 티오펜-카복실산의 아실기인 일반식(I)에 상응하는 9β,11β-옥시도-3,20-디온-1,4-프레그나디엔의 9β,11β-에폭사이드환을 개환시키고 9α-불소 또는 -염소 및 11β-하이드록시 그룹을 동시에 부가 반응시켜 각각 목적하는 일반식(I)의 9α-클로로-11β-하이드록시- 또는 9α-플루오로-11β-하이드록시-화합물을 제조함을 특징으로 하는 상기 1의 제법 C에 따른 방법.
  7. A와 Z'가 모두 수소이고 X는 수소 또는 α-불소이고 Z는 수소 또는 불소이고 X는 메틸, 특히 α-메틸이고 V는 푸란- 또는 티오펜-카복실산의 아실기이고 G는 상기 -QV2에 저의된 아실기인 일반식(I)에 상응하는 3,11,20-트리옥소-1,4-프레그나디엔의 C-11 위치를 환원시킴을 특징으로하는 상기 1의 제법 C에 따른 방법.
  8. A와 Z'가 모두 수소이고 X가 할로겐 특히 불소이고 Z는 수소 또는 불소이고 W는 메틸 특히 α-메틸이고 21-아실레이트가 Q와 V2가 상기 일반식(I)에서 정의된 -QV2인 일반식(I)에 상용하는 11β-보호된 하이드록시-17α-푸로 에이트-(또는 17α-레노에이트)-21-아실레이트의 11위치를 가수분해시켜 목적하는 일반식(I)의 17α,21-디에스테르를 제조함을 특징으로 하는 상기 1의 제법 B에 따른 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR8200374A 1981-02-02 1982-01-29 스테로이드의 방향성 헤테로사이클릭 에스테르 및 이의 제조방법 KR890000761B1 (ko)

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US23076381A 1981-02-02 1981-02-02
US230763 1994-04-21

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KR890000761B1 KR890000761B1 (ko) 1989-04-05

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EP (1) EP0057401B1 (ko)
JP (1) JPS57146800A (ko)
KR (1) KR890000761B1 (ko)
AT (1) ATE8790T1 (ko)
AU (1) AU549102B2 (ko)
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CA (1) CA1177822A (ko)
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JPS57146800A (en) 1982-09-10
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ATE8790T1 (de) 1984-08-15
DE3260474D1 (en) 1984-09-06
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IL64885A (en) 1985-05-31
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