KR840001560A - 벤조복소 환상 화합물의 제조방법 - Google Patents

벤조복소 환상 화합물의 제조방법 Download PDF

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KR840001560A
KR840001560A KR1019820003945A KR820003945A KR840001560A KR 840001560 A KR840001560 A KR 840001560A KR 1019820003945 A KR1019820003945 A KR 1019820003945A KR 820003945 A KR820003945 A KR 820003945A KR 840001560 A KR840001560 A KR 840001560A
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hydrogen
general formula
protecting group
methyl
represented
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KR1019820003945A
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KR890000380B1 (ko
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쉬롬 쿠르트 (외 3)
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페터 베에르호프,기셀라 베흘만
베링거 인겔하임 케이지
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/341,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/361,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Feed For Specific Animals (AREA)
  • Fodder In General (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

내용 없음

Description

벤조복소 환상 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. (a) 하기 일반식(Ⅴ)로 표시되는 화합물을 환원시키고, 필요에 따라서는 여전히 존재하는 보호기를 이어서 제거시키거나; 또는 (b) 하기 일반식(XII)로 표시되는 페닐 글리옥살 또는 헤미아세탈을 하기 일반식(ⅩⅢ)으로 표시되는 아민과 환원적 아민화 조건하에 반응시키고, 필요에 따라서는 여전히 존재하는 보호기를 이어서 제거시키거나; 또는 (c) 제거해야 할 1개 이상의 보호기가 존재하는 하기 일반식(ⅩⅥ)으로 표시되는 화합물로부터 보호기를 상법에 의해 제거시킨 다음; (a), (b) 또는 (c)에서 생성되는 화합물을 필요에 따라서는 상법에 의해 그의 거울상 이성체, 가능한 그의 거울상 이성체의 부분입체 이성체 쌍으로 분할시키고 맨처음에 얻어지는 염기를 산부가염으로 전환시키거나, 또는 맨처음에 얻어지는 산부가염을 염기 또는 다른산의 염으로 전환시킴을 특징으로 하는 하기 일반식(Ⅰ)로 표시되는 복소환상 화합물을 제조하는 방법.
    상기 식들에 있어서, A는 단일결합,또는 -CH2-CH2-를 나타내고; R1은 OH, O-아실, 염소, 또는 수소를 나타내며; R2는 수소, 메틸 또는 에틸을 나타내며; R3로 표시되는 일반식(Ⅱ) 또는로 표시되는 일반식(Ⅲ)을 나타내며;
    여기에서, m은 2, 3 또는 4를 나타내며; n은 1, 2 또는 3을 나타내며; R4는 수소 또는 저급알킬을 나타내며; R5는 수소 또는 저급알킬을 나타내며, R4가 수소일 경우는 R5는 또한 페닐을 나타내며; R6는 수소 또는 메틸을 나타내며; R7은 수소 또는 메틸을 나타내며; R8은 수소 또는 메틸을 나타내며; R9는 수소 Ar, OAr 또는 NH-CO-Ar(Ar은또는임)을 나타내며;
    R10, R11, R12는 서로 동일 또는 상이할 수 있으며, 수소, 히드록시, 메틸, 메톡시, 할로겐, 메틸렌-디옥시, NH-R13(R13은 수소, 아실 또는 저급알킬술포닐임) 또는 CONH2를 나타내며; 존재할 수도 있는 페놀성 OH기는, 수소첨가 분해에 의해 이탈가능한 보호기로 보호될 수 있으며; A는 -CHO 또는 -CH(OH)-O-저급알킬기를 나타내며; R1'는 R1또는 수소첨가 분해에 의해 이탈가능한 보호기로 보호된 OH기를 나타내며; R3'는 R3를 나타내나, R3중 OH기는 수소 첨가분해에 의해 보호될 수 있으며; R'는 수소 또는 수소첨가 분해에 의해 이탈가능한 보호기를 나타낸다.
  2. 제1항에 있어서, 5'-히드록시-8'-(1-히드록시-2-이소프로필아미노-부틸)-2H-1, 4-벤졸사진-3-(4H)-온 및 그의 염을 제조하는 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR8203945A 1981-09-01 1982-09-01 벤조 헤테로사이클 화합물의 제조방법 KR890000380B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19813134590 DE3134590A1 (de) 1981-09-01 1981-09-01 Neue benzo-heterocyclen
DE3134590.5 1981-09-01

Publications (2)

Publication Number Publication Date
KR840001560A true KR840001560A (ko) 1984-05-07
KR890000380B1 KR890000380B1 (ko) 1989-03-15

Family

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Family Applications (1)

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KR8203945A KR890000380B1 (ko) 1981-09-01 1982-09-01 벤조 헤테로사이클 화합물의 제조방법

Country Status (25)

Country Link
EP (1) EP0073505B1 (ko)
JP (1) JPS5852278A (ko)
KR (1) KR890000380B1 (ko)
AR (2) AR231976A1 (ko)
AT (1) ATE16703T1 (ko)
AU (1) AU553589B2 (ko)
CA (1) CA1180012A (ko)
CS (1) CS236679B2 (ko)
DD (1) DD204477A5 (ko)
DE (2) DE3134590A1 (ko)
DK (1) DK158664C (ko)
ES (3) ES515380A0 (ko)
FI (1) FI78475C (ko)
GB (1) GB2106105B (ko)
GR (1) GR77275B (ko)
HU (1) HU186112B (ko)
IE (1) IE53615B1 (ko)
IL (1) IL66683A0 (ko)
NO (1) NO157738C (ko)
NZ (1) NZ201777A (ko)
PL (1) PL139375B1 (ko)
PT (1) PT75478A (ko)
SU (1) SU1149876A3 (ko)
YU (1) YU42794B (ko)
ZA (1) ZA826349B (ko)

Families Citing this family (22)

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Publication number Priority date Publication date Assignee Title
US4554284A (en) * 1984-09-12 1985-11-19 Smithkline Beckman Corporation 7-(2-Aminoethyl)-1,3-benzthia- or oxa-zol-2(3H)-ones
DE3743265A1 (de) * 1987-12-19 1989-06-29 Boehringer Ingelheim Kg Neue ammoniumverbindungen, ihre herstellung und verwendung
TW372967B (en) * 1994-12-27 1999-11-01 Kanebo Ltd 1,4 benzoxazine derivative, pharmaceutical composition containing the same and use thereof
DE10253282A1 (de) * 2002-11-15 2004-05-27 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von chronisch obstruktiver Lungenerkrankung
US7056916B2 (en) 2002-11-15 2006-06-06 Boehringer Ingelheim Pharma Gmbh & Co. Kg Medicaments for the treatment of chronic obstructive pulmonary disease
PE20040950A1 (es) 2003-02-14 2005-01-01 Theravance Inc DERIVADOS DE BIFENILO COMO AGONISTAS DE LOS RECEPTORES ADRENERGICOS ß2 Y COMO ANTAGONISTAS DE LOS RECEPTORES MUSCARINICOS
ATE421322T1 (de) * 2003-04-04 2009-02-15 Novartis Pharma Gmbh Chinolin-2-on-derivate zur behandlung von erkankungen der atemwege
GB0307856D0 (en) * 2003-04-04 2003-05-14 Novartis Ag Organic compounds
US7307076B2 (en) 2004-05-13 2007-12-11 Boehringer Ingelheim International Gmbh Beta agonists for the treatment of respiratory diseases
EP1789394A1 (de) * 2004-05-13 2007-05-30 Boehringer Ingelheim International Gmbh Hydroxy-substituierte benzkondensierte heterozyklen als betaagonisten zur behandlung von atemwegserkrankungen
US7220742B2 (en) 2004-05-14 2007-05-22 Boehringer Ingelheim International Gmbh Enantiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments
DE102004024453A1 (de) * 2004-05-14 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue langwirksame Bronchodilatoren zur Behandlung von Atemwegserkrankungen
DE102004024452A1 (de) * 2004-05-14 2005-12-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Aerosolformulierung für die Inhalation von Betaagonisten
DE102004024451A1 (de) 2004-05-14 2005-12-22 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pulverformulierungen für die Inhalation, die Enantiomerenreine Betaagonisten enthalten
DE102004024454A1 (de) * 2004-05-14 2005-12-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Enantiomerenreine Betaagonisten, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
US7745621B2 (en) 2004-05-14 2010-06-29 Boehringer Ingelheim International Gmbh Long acting bronchodilators for the treatment of respiratory diseases
AU2006281449B2 (en) 2005-08-15 2013-01-31 Boehringer Ingelheim International Gmbh Method for producing betamimetics
US20070088030A1 (en) 2005-10-10 2007-04-19 Barbara Niklaus-Humke Aerosol formulations for the inhalation of beta-agonists
GB0602778D0 (en) 2006-02-10 2006-03-22 Glaxo Group Ltd Novel compound
US20100222336A1 (en) * 2006-08-07 2010-09-02 Boehringer Ingelheim International Gmbh Single enantiomer beta-agonists, methods for the production thereof and the use thereof as medication
UY30543A1 (es) * 2006-08-18 2008-03-31 Boehringer Ingelheim Int Formulacion de aerosol para la inhalacion de beta- agonistas
KR101456872B1 (ko) * 2007-01-25 2014-10-31 베링거 인겔하임 인터내셔날 게엠베하 베타미메틱의 제조방법

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2035749A1 (ko) * 1969-02-06 1970-12-24 Bellon Labor Sa Roger
CA1041523A (en) * 1974-06-19 1978-10-31 Queen's University Preparation of 1-oxapenicillins and novel intermediates therefor

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CA1180012A (en) 1984-12-27
DE3267702D1 (en) 1986-01-09
HU186112B (en) 1985-06-28
ES521871A0 (es) 1984-06-16
FI822985A0 (fi) 1982-08-30
YU42794B (en) 1988-12-31
JPS5852278A (ja) 1983-03-28
DK158664C (da) 1991-01-14
FI822985L (fi) 1983-03-02
NO157738C (no) 1988-05-11
AU553589B2 (en) 1986-07-24
PL139375B1 (en) 1987-01-31
ZA826349B (en) 1984-04-25
ES521870A0 (es) 1984-01-16
EP0073505A1 (de) 1983-03-09
ES8405778A1 (es) 1984-06-16
IE822105L (en) 1983-03-01
EP0073505B1 (de) 1985-11-27
JPH035392B2 (ko) 1991-01-25
IE53615B1 (en) 1988-12-21
YU194982A (en) 1984-12-31
SU1149876A3 (en) 1985-04-07
ES8308318A1 (es) 1983-08-16
NO157738B (no) 1988-02-01
NZ201777A (en) 1985-08-30
CS236679B2 (en) 1985-05-15
DD204477A5 (de) 1983-11-30
AR231977A1 (es) 1985-04-30
NO822932L (no) 1983-03-02
PL238077A1 (en) 1984-04-09
ATE16703T1 (de) 1985-12-15
AR231976A1 (es) 1985-04-30
GB2106105A (en) 1983-04-07
GR77275B (ko) 1984-09-11
FI78475C (fi) 1989-08-10
DK158664B (da) 1990-07-02
PT75478A (en) 1982-09-01
ES8402279A1 (es) 1984-01-16
FI78475B (fi) 1989-04-28
DK389082A (da) 1983-03-02
IL66683A0 (en) 1982-12-31
AU8787482A (en) 1983-03-10
ES515380A0 (es) 1983-08-16
GB2106105B (en) 1985-07-10
DE3134590A1 (de) 1983-03-10
KR890000380B1 (ko) 1989-03-15

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