KR830005263A - 17α-아실록시-5β-코르티코이드 및 17α-아실록시-5α-코르티코이드의 제조방법 - Google Patents

17α-아실록시-5β-코르티코이드 및 17α-아실록시-5α-코르티코이드의 제조방법 Download PDF

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KR830005263A
KR830005263A KR1019810000285A KR810000285A KR830005263A KR 830005263 A KR830005263 A KR 830005263A KR 1019810000285 A KR1019810000285 A KR 1019810000285A KR 810000285 A KR810000285 A KR 810000285A KR 830005263 A KR830005263 A KR 830005263A
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KR1019810000285A
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KR850001208B1 (ko
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에모리 에이아 도날드
알빈 쉬라겔 카알
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제라아드 토마스
디 엎죤 캄파니
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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
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0053—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 substituted in position 17 alfa not substituted in position 16
    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0061—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 substituted in position 17 alfa substituted in position 16
    • C07J5/0069—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa substituted in position 16
    • C07J7/0055—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • C07J71/0015—Oxiranes at position 9(11)

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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

내용 없음

Description

17α-아실록시-5β-코르티코이드 및 17α-아실록시-5α-코르티 코이드의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. 하기 구조식(IA)의 화합물을 수첨촉매 존재하에 수소첨가하고
  2. 5α-이성체로부터 5β-이성체를 부리하여 하기 구조식(I)의 5β-스테로이드를 제조하는 방법 :
    상기식에서 R2는 수소, 불소 또는 염소원자 또는 메틸기이고; R6는 수소, 불소 또는 염소원자 또는 메틸기이고; R7은 수소, 불소 또는 염소원자이고; R9은 수소, 불소 또는 염소원자이고, R11은 염소 또는 산소원자 또는 수산기이고; R11이 염소원자 또는 수산기일때,
    R11과 C11사이의는 β위치에서 단일 결합이고,
    R11이 산소원자일 때, R11과 C11사이의는 이중 결합이고; R16α는 수소, 불소 또는 염소 원자 또는 메틸기이고; R16β가 수소원자 또는 메탈기이고(단, R16α 또는 R16β중 하나가 수소원자일때 임); R17이 탄소수 1-6의 알킬, 페닐, P-메틸페닐, P-카르복사페닐 또는 P-카르보알콕시페닐; R21은 수소, 불소, 염소 또는 브롬원자 또는 -OR21a또는 -OSO2CH3기이고 (R21a는 수소원자, -COR21b또는 -PO(OH)2및 약리적으로 수용할 수 있는 그의 염임); R21b가 탄소수 1-6의 알킬, 페닐, P-메틸페닐, 또는 P-카르복시페닐, P-카르보알콕시페닐, -CH2CH2COOH 및 약리적으로 수용할 수 있는 그의 염일때은 단일 또는 이중결합이며 "∼"는 부착기가 α 또는β위치에 있을 수 있다는 것을 뜻한다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810000285A 1980-01-31 1981-01-30 17α-아실옥시-5β-코르티코이드 및 17α-아실옥시-5α-코르티코이드의 제조방법 KR850001208B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US117401 1980-01-31
US117,401 1980-01-31
US06/117,401 US4318853A (en) 1980-01-31 1980-01-31 9β,11β-Epoxy-5β-corticoids

Publications (2)

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KR830005263A true KR830005263A (ko) 1983-08-03
KR850001208B1 KR850001208B1 (ko) 1985-08-20

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US (1) US4318853A (ko)
JP (1) JPS56122398A (ko)
KR (1) KR850001208B1 (ko)
AU (1) AU538883B2 (ko)
BE (1) BE887323A (ko)
CA (1) CA1155108A (ko)
CH (1) CH644614A5 (ko)
DE (1) DE3102397A1 (ko)
DK (1) DK39281A (ko)
ES (1) ES8300342A1 (ko)
FR (1) FR2475048A1 (ko)
GB (1) GB2070016B (ko)
GR (1) GR73511B (ko)
IT (1) IT1193576B (ko)
NL (1) NL8100467A (ko)
PH (2) PH16525A (ko)
SE (1) SE8100563L (ko)
ZA (1) ZA8118B (ko)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3243482A1 (de) * 1982-11-22 1984-05-24 Schering AG, 1000 Berlin und 4709 Bergkamen Neue 6(alpha)-methylkortikoide, ihre herstellung und verwendung
ES2041245T3 (es) * 1985-10-23 1993-11-16 The Upjohn Company Esteroides angioestaticos.
NL8900507A (nl) * 1989-03-02 1990-10-01 Philips Nv Versterkerschakeling met verzadigingsdetectie.
CA2139549A1 (en) * 1994-01-28 1995-07-29 Kazumi Ogata Corticoid derivatives and pharmaceutical and cosmetic compositions
GB2302807A (en) * 1995-07-04 1997-02-05 Surtech Int Ltd Method and composition for treating atopic eczema
DE19737348C2 (de) * 1997-08-27 2002-07-25 Dan-Gabriel Vulpescu Neue Clindamycin und Clotrimazol enthaltende pharmazeutische Zusammensetzung
EP3656385A1 (en) 2008-05-28 2020-05-27 ReveraGen BioPharma, Inc. Non-hormonal steroid modulators of nf-kb for treatment of disease
WO2011127048A2 (en) 2010-04-05 2011-10-13 Validus Biopharma NON-HORMONAL STEROID MODULATORS OF NF-ĸB FOR TREATMENT OF DISEASE
CN102225959B (zh) * 2011-04-29 2012-11-07 中国科学院上海有机化学研究所 一种16β-甲基-17α-羟基孕甾-3,20-二酮化合物及其合成方法
US10799514B2 (en) 2015-06-29 2020-10-13 Reveragen Biopharma, Inc. Non-hormonal steroid modulators of NF-kappa beta for treatment of disease
US11382922B2 (en) 2019-03-07 2022-07-12 Reveragen Biopharma, Inc. Aqueous oral pharmaceutical suspension compositions

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2831874A (en) * 1954-04-20 1958-04-22 Gnrd Patent Holdings Ltd Improvements in the preparation of 17:21-diacyloxy-2:4-dibromo-3:11:20-triketoallopregnanes
US2854465A (en) * 1955-02-18 1958-09-30 Ciba Pharm Prod Inc Process for the manufacture of halogen-pregnanes and dehalogenation products thereof
CH429716A (de) * 1961-06-24 1967-02-15 Vismara Francesco Spa Verfahren zur Herstellung von 17a-Acyloxy-21-hydroxy-Steroiden
US3681410A (en) * 1970-08-07 1972-08-01 Syntex Corp Process for preparing 17{60 -hydroxy-20-keto and 17{60 ,21-dihydroxy-20-keto pregnanes and derivatives and intermediates thereof

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GR73511B (ko) 1984-03-07
CH644614A5 (de) 1984-08-15
SE8100563L (sv) 1981-08-01
DE3102397A1 (de) 1981-12-24
NL8100467A (nl) 1981-09-01
KR850001208B1 (ko) 1985-08-20
AU538883B2 (en) 1984-08-30
AU6651381A (en) 1981-08-06
FR2475048B1 (ko) 1984-11-16
ZA8118B (en) 1982-01-27
JPS56122398A (en) 1981-09-25
CA1155108A (en) 1983-10-11
IT1193576B (it) 1988-07-08
GB2070016B (en) 1983-09-14
GB2070016A (en) 1981-09-03
DK39281A (da) 1981-08-01
ES498938A0 (es) 1982-11-01
ES8300342A1 (es) 1982-11-01
BE887323A (fr) 1981-07-30
IT8119360A0 (it) 1981-01-27
FR2475048A1 (fr) 1981-08-07
PH16525A (en) 1983-11-10
PH19579A (en) 1986-05-26
US4318853A (en) 1982-03-09

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