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KR880001625A - 탁솔 유도체, 그 제법 및 그들을 함유한 약제학적 조성물 - Google Patents

탁솔 유도체, 그 제법 및 그들을 함유한 약제학적 조성물 Download PDF

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Publication number
KR880001625A
KR880001625A KR1019870007752A KR870007752A KR880001625A KR 880001625 A KR880001625 A KR 880001625A KR 1019870007752 A KR1019870007752 A KR 1019870007752A KR 870007752 A KR870007752 A KR 870007752A KR 880001625 A KR880001625 A KR 880001625A
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South Korea
Prior art keywords
tert
hydrogen
butoxycarbonylamino
hydroxy
taxol derivative
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KR1019870007752A
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English (en)
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KR950006153B1 (ko
Inventor
꼴랭 미쉘
괴나르 다니엘
괴리뜨-보에즐렝 프랑소와즈
뽀띠에 삐에르
Original Assignee
쟈끄 삘라르
로오느-푸우랜크 상뜨
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Application filed by 쟈끄 삘라르, 로오느-푸우랜크 상뜨 filed Critical 쟈끄 삘라르
Publication of KR880001625A publication Critical patent/KR880001625A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • 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
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

탁솔 유도체, 그 제법 및 그들을 함유한 약제학적 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(I)의탁솔 유도체와 그 입체 이성체 및 그들의 혼합물 :
    상기식에서 R은 수소나 아세틸이고, R1과 R2중 하나는 히드록시이고, 다른 하나는 3차-부톡시카르보닐아미노이다.
  2. 제1항에 있어서, R이 수소이고, R1이 히드록시이고, R2가 3차-부톡시카르보닐아미노이며 2'R, 3'S의 배치를 갖는 탁솔 유도체.
  3. 제1항에 있어서, R이 수소이고, R1이 히드록시이고, R2가 3차-부톡시카르보닐아미노이며 2'S, 3'R의 배치를 갖는 탁솔 유도체.
  4. 제1항에 있어서, R이 수소이고, R1이 3차-부톡시카르보닐아미노이고, R2가 히드록시이며 2'R, 3'S의 배치를 갖는 탁솔 유도체.
  5. 제1항에 있어서, R이 수소이고, R1이 3차-부톡시카르보닐아미노이고 R2가 히드록시이며 2'S, 3'R의 배치를 갖는 탁솔 유도체.
  6. 0-40℃에서 사산화 오스뮴과 질산은의 존재하에 유기 용매속에서, 3차-부틸 N-클로로카르바메이트의 나트륨염을 하기 일반식(III)의 화합물과 반응시키고, 30-60℃에서 아세트산의 존재하에 아연을 사용해 하기 일반식(IV)의 생성물에서 2,2,2-트리클로로에톡시카르보닐기(들)을 수소로 대치하고, 얻어진 탁솔 유도체를 분리하는 것으로 구성되는, 제1항의 탁솔 유도체를 제조하는 방법 :
    (상기식에서 R'는 아세틸이나 2,2,2-트리클로로에톡시카르보닐이다.)
    (상기식에서 R'는 상기에 정의한 바와 같고 R1과 R2는 제1항에서 전의한 바와 같다.)
  7. 제6항에 있어서, 유기 용매가 아세토니트릴이고 사산화 오스뮴이 3차-부탄올내 용액으로 사용되는 방법.
  8. 신남산을 하기 일반식(V)의 화합물과 반응시키는 것으로 구성되는 하기 일반식(III)의 화합물의 제조방법;
    (상기식에서 R'는 아세틸이나 2,2,2-트리클로로에톡시카르보닐이다.)
  9. 제8항에 있어서, 반응이 60-90℃의 방향족 탄화수소속에서 카르보디아미드와 같은 응축제 또는 반응성 탄산염 및 활성제의 존재하에 효과적으로 수행되는 방법.
  10. 하나 이상의 약제학적으로 허용되는 비활성 또는 생리학적으로 활성인 희석제나 보조네와 조합된 제1항 내지 제5항중 어느 하나의 탁솔 유도체를 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870007752A 1986-07-17 1987-07-16 탁솔 유도체, 그 제법 및 그들을 함유한 약제학적 조성물 KR950006153B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR8610400 1986-07-17
FR8610400A FR2601675B1 (fr) 1986-07-17 1986-07-17 Derives du taxol, leur preparation et les compositions pharmaceutiques qui les contiennent
FR86/10400 1986-07-17

Publications (2)

Publication Number Publication Date
KR880001625A true KR880001625A (ko) 1988-04-25
KR950006153B1 KR950006153B1 (ko) 1995-06-09

Family

ID=9337506

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019870007752A KR950006153B1 (ko) 1986-07-17 1987-07-16 탁솔 유도체, 그 제법 및 그들을 함유한 약제학적 조성물

Country Status (15)

Country Link
US (1) US4814470A (ko)
EP (1) EP0253738B1 (ko)
JP (1) JPH0651689B2 (ko)
KR (1) KR950006153B1 (ko)
AT (1) ATE49962T1 (ko)
AU (1) AU591309B2 (ko)
CA (1) CA1278304C (ko)
DE (1) DE3761562D1 (ko)
ES (1) ES2012809B3 (ko)
FR (1) FR2601675B1 (ko)
GR (1) GR3000287T3 (ko)
LU (1) LU88712I2 (ko)
MX (1) MX9203385A (ko)
NL (1) NL960002I2 (ko)
ZA (1) ZA875179B (ko)

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