KR830006248A - 3, 1-벤조아진-2-온의 제조방법 - Google Patents

3, 1-벤조아진-2-온의 제조방법 Download PDF

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Publication number
KR830006248A
KR830006248A KR1019810002523A KR810002523A KR830006248A KR 830006248 A KR830006248 A KR 830006248A KR 1019810002523 A KR1019810002523 A KR 1019810002523A KR 810002523 A KR810002523 A KR 810002523A KR 830006248 A KR830006248 A KR 830006248A
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South Korea
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alkyl
group
hydrogen
methyl
fluorine
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KR1019810002523A
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English (en)
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KR850000755B1 (en
Inventor
멘트럽 안톤
쉬롬 쿠르트
렌스 에른스트-오토
호 에프케 볼프강
가이다 볼프람
스트레일레르 일쎄
푸그너 아르민
Original Assignee
오토 핑케, 기셀라 베홈만
씨. 에이취. 베링거죤
기셀라 베홈만
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Application filed by 오토 핑케, 기셀라 베홈만, 씨. 에이취. 베링거죤, 기셀라 베홈만 filed Critical 오토 핑케, 기셀라 베홈만
Publication of KR830006248A publication Critical patent/KR830006248A/ko
Priority to KR1019850001963A priority Critical patent/KR850000754B1/ko
Priority to KR1019850001965A priority patent/KR850000741B1/ko
Application granted granted Critical
Publication of KR850000755B1 publication Critical patent/KR850000755B1/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

내용 없음

Description

3, 1-벤조아진-2-온의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 라세메이트, 임의적으로는 정반대의 투공성이성체 및 개개의 광학적 대칭체 형태로 각각 유리염기로서 또는 산부가염으로서 존재하는 다음 구조식(I)의 3,1-벤조아진-2-온 화합물.
    상기 구조식을 설명하면
    R1및 R2는 같거나 다르며, 수소 또는 (C1-C4) 알킬을 나타내고
    R3및 R4는 같거나 다르며, 수소, 불소, 염소, 하이드록시, 메틸, 에틸, (C1-C4) 알콕시를 나타내거나 또는 모두 메틸렌디옥시를 나타내고
    R5및 R6는 같거나 다르며, 수소 또는 메틸을 나타내고
    R7은 다음 기를 나타내고
    상기 기를 설명하면
    R은 수소 또는 (C1-C4) 알킬이며,
    R8은 불소, 염소, (C1-C4) 알킬, (C1-C4) 알킬티오, 하이드록시메틸 또는 CONHR11, SO2NHR11, OR2그룹중 하나, 메톡시카보닐, 에톡시카보닐 또는 NHSO2CH3를 나타내고
    R9는 수소, 불소, 염소 또는 OR12를 나타내고
    R10는 수소, 아미노, 메틸, 메톡시 또는 염소를 나타내고
    R11는 수소, 메틸, 에틸 또는 하이드록시에틸을 나타내고
    R12는 수소, (C1-C4) 알킬, (C1-C4) 알킬-CO, 아릴-CH2또는 아릴-CO를 나타내고 및
    n은 1,2 또는 3을 나타낸다.
  2. 다음과 같은 특성을 갖는 청구범위 제1항에 의한 화합물.
    R1/R2:CH3/CH3또는 CH3/H
    R3:H, OH, OCH3
    R4:H
    R5/R6:CH3/CH3, CH3/H 또는 H/H
    R7:상기 정의한 바와 같으며
    R:H, CH3, C2H5,
    R8:CONHR11, SO2NHR11, NHSO2CH3, OR12, F, Cl, COO 알킬, CH2OH
    R9:OR12, F, Cl, H
    R10:H, NH2, CH3, Cl,
    R11:H, CH3, C2H5
    R12:H, 아릴-CH2, 알킬-CO,
    n:1 또는 2
  3. 통상의 부형약제 및/또는 담체를 갖는 청구범위 제(1)항 또는 제(2)항 모두에 의한 화합물을 함유하는데 특성있는 약학 조성물.
  4. 저혈압제, 토콜리성제, 기관지용해제, 혈관화장제 및 카디성 약학제로서 청구범위 제(1)항 또는 제(2)항에 의한 화합물의 용도.
  5. (가) 다음 구조식(Ⅱ)의 화합물을 환원하거나, (나) 다음 구조식(Ⅲ)의 화합물을 다음 구조식(Ⅳ)의 화하불로 환원성 알킬화에 의해 제조하거나, 또는 (다) 다음 구조식(Ⅶ)의 화합물로부터 보호기 R14를 제거하거나 또는 (라) 구조식(Ⅸ)의 화합물을 다음 구조식(X)의 아민과 반응시켜서 제조하며, 필요한 경우, (가)-(라)에 따라 수득된 생성물을 정반대의 투공이성체쌍으로 또는 개개의 광학적 대칭체로 재용해하며 및/또는 최초에 수득된 염기를 산부가염으로 전환시키면서 최초에 수득된 산부가염을 유리염기로 전환시킴을 특징으로 하는 상기 청구범위 제1항 또는 제2항에 의한 화합물의 제조방법.
    상기 구조식을 설명하면,
    R, R1-R11은 상기 정의한 바와 같으며
    R13은 C1-C4알킬을 나타내며
    R14는 임의로 치환된 벤질, CO-(C1-C4-알킬) 또는 CO-알킬을 나타내며, 및
    R15는 임의로 치환된 알킬 또는 아르알킬을 나타낸다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR8102523A 1980-07-12 1981-07-11 Process for preparing 3,1-benzoxazin-2-ones and acid addition salts thereof KR850000755B1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
KR1019850001963A KR850000754B1 (ko) 1980-07-12 1985-03-25 3, 1-벤즈옥사진-2-온 및 이의 산부가염의 제조방법
KR1019850001965A KR850000741B1 (ko) 1980-07-12 1985-03-25 3,1-벤즈옥사진-2-온 및 이의 산 부가염의 제조방법

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19803026534 DE3026534A1 (de) 1980-07-12 1980-07-12 3,1-benzoxazin-2-one, ihre herstellung und verwendung

Related Child Applications (2)

Application Number Title Priority Date Filing Date
KR1019850001965A Division KR850000741B1 (ko) 1980-07-12 1985-03-25 3,1-벤즈옥사진-2-온 및 이의 산 부가염의 제조방법
KR1019850001963A Division KR850000754B1 (ko) 1980-07-12 1985-03-25 3, 1-벤즈옥사진-2-온 및 이의 산부가염의 제조방법

Publications (2)

Publication Number Publication Date
KR830006248A true KR830006248A (ko) 1983-09-20
KR850000755B1 KR850000755B1 (en) 1985-05-25

Family

ID=6107085

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Application Number Title Priority Date Filing Date
KR8102523A KR850000755B1 (en) 1980-07-12 1981-07-11 Process for preparing 3,1-benzoxazin-2-ones and acid addition salts thereof

Country Status (25)

Country Link
US (1) US4341778A (ko)
EP (1) EP0043940B1 (ko)
JP (1) JPS5748975A (ko)
KR (1) KR850000755B1 (ko)
AT (1) ATE9336T1 (ko)
AU (1) AU540916B2 (ko)
CA (1) CA1165317A (ko)
DD (1) DD202018A5 (ko)
DE (2) DE3026534A1 (ko)
DK (1) DK149851C (ko)
ES (4) ES503837A0 (ko)
FI (1) FI74703C (ko)
GB (1) GB2080296B (ko)
GR (1) GR74333B (ko)
HK (1) HK98286A (ko)
HU (1) HU183515B (ko)
IE (1) IE52508B1 (ko)
IL (1) IL63285A (ko)
NO (1) NO158578C (ko)
NZ (1) NZ197678A (ko)
PH (1) PH17425A (ko)
PT (1) PT73338B (ko)
SG (1) SG77686G (ko)
YU (1) YU170181A (ko)
ZA (1) ZA814687B (ko)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4446319A (en) * 1981-04-28 1984-05-01 Takeda Chemical Industries, Ltd. Aminocyclitols and their production
JPS62238288A (ja) * 1986-04-04 1987-10-19 Nippon Tokushu Noyaku Seizo Kk 環状カルバメ−ト及び農園芸用殺菌剤
FR2636065B1 (fr) * 1988-09-08 1993-05-07 Fabre Sa Pierre Nouveaux derives de dihydro-2,3 arylacoylaminoalcoyl-3 4h-benzoxazine-1,3 ones-4, leur preparation et leur application en tant que medicaments utiles en therapeutique
JP2807577B2 (ja) * 1990-06-15 1998-10-08 エーザイ株式会社 環状アミド誘導体
FR2680172B1 (fr) * 1991-08-05 1993-11-19 Fabre Medicament Pierre Nouvelles piperazinylalcoyl-3 dihydro-2,3 4h-benzoxazine-1,3 ones-4 substituees, leur preparation et leur application en therapeutique.
EP0805681A4 (en) * 1995-01-24 1998-05-06 Merck & Co Inc TOCOLYTIC ANTAGONISTS OF OXYTOCIN RECEPTORS
US5874430A (en) * 1996-10-02 1999-02-23 Dupont Pharmaceuticals Company 4,4-disubstitued-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same
DE102004003428A1 (de) * 2004-01-23 2005-08-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue langwirksame Beta-2-Agonisten, und deren Verwendung als Arzneimittel
EP1844768A1 (en) * 2005-01-19 2007-10-17 Dainippon Sumitomo Pharma Co., Ltd. Aromatic sulfone compound as aldosterone receptor modulator
DE102005008921A1 (de) * 2005-02-24 2006-08-31 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittel zur Behandlung von Atemwegserkrankungen
US7423146B2 (en) * 2005-11-09 2008-09-09 Boehringer Ingelheim International Gmbh Process for the manufacturing of pharmaceutically active 3,1-benzoxazine-2-ones
UY30552A1 (es) * 2006-08-22 2008-03-31 Boehringer Ingelheim Int Combinaciones farmacologiicas en base a derivados sustituidos de la n-(5-{2-[1,1-dimetil-propilamino]-1-hidroxi-metil}-2-hidroxi-fenil)-metansulfonamida y aplicaciones
PE20080610A1 (es) * 2006-08-22 2008-07-15 Boehringer Ingelheim Int Nuevos beta-agonistas enantiomericamente puros, procedimientos para su preparacion y uso como medicamentos
PE20080425A1 (es) * 2006-08-22 2008-06-16 Boehringer Ingelheim Int Formulacion aerosol para la inhalacion de beta-agonistas
US20100233268A1 (en) * 2006-08-22 2010-09-16 Boehringer Ingelheim International Gmbh Powder formulations for inhalation containing enantiomerically pure beta-agonists
EP2093219A1 (de) 2008-02-22 2009-08-26 Boehringer Ingelheim International Gmbh Kristalline, enantiomerenreine Salzform eines Betamimetikums und dessen Verwendung als Arzneimittel

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3526621A (en) * 1966-08-03 1970-09-01 Farmaceutical Italia Soc Substituted 3,1-benzoxazin-2-one
DE2609645A1 (de) * 1976-03-09 1977-09-15 Boehringer Sohn Ingelheim Aminoalkylheterocyclen
US4163053A (en) * 1977-12-27 1979-07-31 Schering Corporation Anti-hypertensive 5-[2-(substituted anilinoalkylamino)-1-hydroxyalkyl]salicylamides
FI791727A (fi) * 1978-06-05 1979-12-06 Ciba Geigy Ag Foerfarande foer framstaellning av n-alkylerade aminoalkoholer
DE2833140A1 (de) * 1978-07-28 1980-02-07 Boehringer Sohn Ingelheim Neue n-substituierte heterocyclen

Also Published As

Publication number Publication date
FI812183L (fi) 1982-01-13
NO158578C (no) 1988-10-05
ES8300725A1 (es) 1982-11-01
HK98286A (en) 1986-12-24
IL63285A0 (en) 1981-10-30
US4341778A (en) 1982-07-27
IL63285A (en) 1985-03-31
GB2080296A (en) 1982-02-03
NZ197678A (en) 1984-12-14
ES508655A0 (es) 1982-11-01
KR850000755B1 (en) 1985-05-25
AU7273181A (en) 1982-09-16
ES8205402A1 (es) 1982-06-01
DE3026534A1 (de) 1982-03-18
DK149851B (da) 1986-10-13
EP0043940A1 (de) 1982-01-20
GB2080296B (en) 1983-09-28
HU183515B (en) 1984-05-28
IE52508B1 (en) 1987-11-25
ES503837A0 (es) 1982-06-01
GR74333B (ko) 1984-06-25
FI74703C (fi) 1988-03-10
ATE9336T1 (de) 1984-09-15
JPS5748975A (en) 1982-03-20
DK306781A (da) 1982-01-13
SG77686G (en) 1987-02-27
EP0043940B1 (de) 1984-09-12
ZA814687B (en) 1983-03-30
YU170181A (en) 1983-10-31
NO812355L (no) 1982-01-13
ES508653A0 (es) 1982-11-01
ES8300726A1 (es) 1982-11-01
ES8300727A1 (es) 1982-11-01
DK149851C (da) 1987-05-04
AU540916B2 (en) 1984-12-06
DE3166003D1 (en) 1984-10-18
PH17425A (en) 1984-08-08
IE811567L (en) 1982-01-12
DD202018A5 (de) 1983-08-24
PT73338B (en) 1983-06-20
ES508654A0 (es) 1982-11-01
PT73338A (de) 1981-08-01
FI74703B (fi) 1987-11-30
NO158578B (no) 1988-06-27
CA1165317A (en) 1984-04-10

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