KR840005427A - Method for preparing carbostyryl derivative - Google Patents

Method for preparing carbostyryl derivative Download PDF

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KR840005427A
KR840005427A KR1019830003040A KR830003040A KR840005427A KR 840005427 A KR840005427 A KR 840005427A KR 1019830003040 A KR1019830003040 A KR 1019830003040A KR 830003040 A KR830003040 A KR 830003040A KR 840005427 A KR840005427 A KR 840005427A
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carbostyryl
lower alkyl
side chain
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KR900006401B1 (en
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미노루 우찌다 (외 2)
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원본 미기재
오오쓰까 세이야꾸 가부시끼 가이샤
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Abstract

내용 없음No content

Description

카르보스티릴 유도체의 제조방법Method for preparing carbostyryl derivative

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음As this is a public information case, the full text was not included.

Claims (54)

하기 일반식으로 표시되는 카르보스티릴 유도체의 제조방법은Method for producing a carbostyryl derivative represented by the following general formula [상기식에서, R1은 수소원자, 저급알킬기, 저급알케닐기, 저급알키닐기 또는 페닐-저급 알키닐기이다; R2는 수소원자, 할로겐원자, 벤질옥시기(치환기로써, 할로겐원자를 가질 수 있는), 수산기, 저급 알킬기 또는 저급알콕시기이다; R3는 수산기, 아미노기[치환기로써, 시클로알킬-저급알킬기(치환기로써, 시클로알킬고리에 카르복시기 또는 저급 알콕시카르보닐기를 가질 수 있는)를 가질 수 있는], 저급 알콜시기, 저급알콕시카르보닐-저급 알콕시기, 벤조일-저급 알콕시기 또는 저급 알카노일옥시-저급 알콕시기이다; R4는 수소원자, 페닐술포닐기(치환기로써 저급 알킬기 또는 할로겐원자를 가질 수 있는), 저급 알킬기, 페닐-저급 알킬기(치환기로써 페닐 고리에 할로겐원자를 가질 수 있는 또는 식 -COR5의 기[상기식에서 R5는 저급알킬기(치환기로써, 아미노기 또는 페닐-저급 알콕시카르보닐아미노기를 가질 수 있는 시클로알킬기(치환기로써, 시클로알킬고리에 아미노-저급알킬기 또는 페닐-저급 알콕시카르보닐아미노-저급알킬기를 가질 수 있는), 페닐기(페닐 고리에 할로겐원자, 저급 알킬기, 저급 알콕시기, 니트로기, 아미노기 및 수산기로 구성되는 기로부터 선택된 1~3개의 치환기를 가질 수 있는), 페닐-저급 알킬기 치환기로써 페닐고리에 할로겐원자를 가질 수 있는), 또는 질소원자, 산소원자 및 황원자로 구성되는 기로부터 선택된 1 또는 2개의 헤테로 원자를 갖는 5- 또는 6-원 불포화된 헤테로시클릭 고리(상기 헤테로시클릭 고리는 치환기로써 저급 알킬기를 가질 수 있는)]이다; R0는 수소원자 또는 페닐술포닐기(치환기로써, 저급 알킬기 또는 할로겐원자를 가질 수 있는)이다;[Wherein, R 1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a phenyl-lower alkynyl group; R 2 is a hydrogen atom, a halogen atom, a benzyloxy group (which may have a halogen atom as a substituent), a hydroxyl group, a lower alkyl group or a lower alkoxy group; R 3 is a hydroxyl group, an amino group [as a substituent, which may have a cycloalkyl-lower alkyl group (which may have a carboxyl group or a lower alkoxycarbonyl group in the cycloalkyl ring as a substituent)], a lower alcohol group, a lower alkoxycarbonyl-lower alkoxy Group, benzoyl-lower alkoxy group or lower alkanoyloxy-lower alkoxy group; R 4 represents a hydrogen atom, a phenylsulfonyl group (which may have a lower alkyl group or a halogen atom as a substituent), a lower alkyl group, a phenyl-lower alkyl group (which may have a halogen atom in the phenyl ring as a substituent or a group of the formula -COR 5 [ Wherein R 5 is a lower alkyl group (as a substituent, a cycloalkyl group which may have an amino group or a phenyl-lower alkoxycarbonylamino group (as a substituent, an amino-lower alkyl group or a phenyl-lower alkoxycarbonylamino-lower alkyl group in the cycloalkyl ring) Phenyl group (which may have 1 to 3 substituents selected from the group consisting of halogen atoms, lower alkyl groups, lower alkoxy groups, nitro groups, amino groups and hydroxyl groups in the phenyl ring), phenyl-lower alkyl group substituents One or two hetero atoms selected from the group consisting of halogen atoms in the ring), or nitrogen atoms, oxygen atoms and sulfur atoms Is a 5- or 6-membered unsaturated heterocyclic ring having a substituent (where the heterocyclic ring may have a lower alkyl group as a substituent); R 0 is a hydrogen atom or a phenylsulfonyl group (as a substituent, a lower alkyl group or a halogen) May have an atom); A는 저급 알킬렌기이다; n은 0 또는 1이다; 식의 측쇄에서로서 나타낸 탄소-탄소 결합은 단일 또는 이중 탄소-탄소 결합을 의미한다;A is a lower alkylene group; n is 0 or 1; expression In the side chain of Carbon-carbon bonds denoted as mean single or double carbon-carbon bonds; 카르보스티릴골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 단일 또는 이중 결합이다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.]In the carbostyryl skeleton, the carbon-carbon bond between the 3- and 4-positions is a single or double bond; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 하기 일반식으로 표시되는 화합물과Compound represented by the following general formula B-NH-R0 B-NH-R 0 [상기 식에서, B는 하기 일반식의 기,[Wherein B is a group of the following general formula, (상기 식에서, R1,R2,R3,A,n, 측쇄에서로서 표시되는 탄소-탄소 결합 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의된 것과 같다; 식의 측쇄의 치환위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느하나이다), 또는 E의 기호이다(여기서 E는 상기 시클로알킬기가 치환기로써 카르복시기 또는 저급 알콕시 카르보닐기를 가질 수 있는 치환된-시클로알킬-저급알킬기이다)].In which R 1 , R 2 , R 3 , A, n, The carbon-carbon bonds between the 3- and 4-positions in the carbon-carbon bonds and carbostyryl backbones represented as are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton, or a symbol of E (where E is a carboxyl group as the substituent of the cycloalkyl group) Or a substituted-cycloalkyl-loweralkyl group which may have a lower alkoxy carbonyl group). 하기 일반식으로 표시되는 화합물의 반응을 특징으로 한다.It is characterized by the reaction of the compound represented by the following general formula. [상기식에서, D는 R5의 기호 또는 하기식의 기이고[Wherein D is a symbol of R 5 or a group of the formula (상기 식에서, R1,R2,R4,R0,측쇄에서로써 나타낸 탄소-탄소 결합, 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의된 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다)]Wherein R 1 , R 2 , R 4 , R 0 , In the side chain The carbon-carbon bonds shown as and the carbon-carbon bonds between the 3- and 4-positions in the carbostyryl backbone are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton)] 일반식 D-COOH는 기호 B가 하기식의 기이고In general formula D-COOH, symbol B is a group of following formula D가 R5의 기호이고; 각각 B의 기호가 E의 기호이고, D가 하기식의 기일 때 제공된다.D is a symbol of R 5 ; It is provided when each symbol of B is a symbol of E and D is a group of the following formula. 2. 하기 일반식으로 표시되는 화합물과2. a compound represented by the following general formula R3'-OHR 3 '-OH (상기 식에서, R3'은 이미 정의하였다).(Wherein R 3 ' is already defined). 하기 일반식으로 표시되는 화합물의 반응에 의해,By reaction of a compound represented by the following general formula, (상기 식에서, R,R,R,R,측쇄에서로써 나타낸 탄소-탄소 결합 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의한 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느하나이다.]Wherein R, R, R, R, In the side chain The carbon-carbon bonds between the 3- and 4-positions in the carbon-carbon bonds and carbostyryl backbones shown as are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 하기 일반식으로 표시되는 카르보스티릴 유도체의 제조방법.Method for producing a carbostyryl derivative represented by the following general formula. (상기 식에서, R1,R2,R4,R0,측쇄에서로써 나타낸 탄소-탄소 결합 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의한 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다; R3'은 저급 알킬기, 저급 알콕시카르보닐-저급 알킬기, 벤조일-저급 알킬기 또는 저급알카노일옥시-저급 알킬기이다.]Wherein R 1 , R 2 , R 4 , R 0 , In the side chain The carbon-carbon bonds between the 3- and 4-positions in the carbon-carbon bonds and carbostyryl backbones shown as are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton; R 3 ′ is a lower alkyl group, lower alkoxycarbonyl-lower alkyl group, benzoyl-lower alkyl group or lower alkanoyloxy-lower alkyl group.] 3. 하기 일반식으로 표시되는 화합물을 가수 분해하여3. Hydrolyze the compound represented by the following general formula 상기 식에서, R1,R2,및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의한 것과 같다; R은 식의 기(여기서 R6및 R8각각 저급 알킬기이다; R7은 저급 알카노일기이다) 또는 식의 기(여기서 R3및 R4는 상기에 정의한 것과 같고; R3가 수신기, R4가 수소원자가 아닐 때 제공된다); 식-(A)n-R의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.]Wherein, R 1 , R 2 , And the carbon-carbon bond between the 3- and 4-positions in the carbostyryl backbone is as defined above; R is an expression R 6 and R 8 are each lower alkyl group; R 7 is a lower alkanoyl group, or Wherein R 3 and R 4 are as defined above; provided when R 3 is a receiver and R 4 is not a hydrogen atom; The substitution position of the side chain of formula- (A) n- R is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 하기 일반식으로 표시되는 카르보스티릴 유도체의 제조방법.Method for producing a carbostyryl derivative represented by the following general formula. [상기 식에서, R1,R2,측쇄에서로써 나타낸 탄소-탄소 결합 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 상기에 정의한 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.][Wherein, R 1 , R 2 , In the side chain The carbon-carbon bonds between the 3- and 4-positions in the carbon-carbon bonds and carbostyryl backbones shown as are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 4. 하기 일반식으로 표시되는 화합물과4. Compound represented by the following general formula R4'―XR 4 ' ―X [상기 식에서, R4'은 이미 정의한 것과 같고; X는 할로겐원자이다.][Wherein R 4 ′ is as defined above; X is a halogen atom.] 하기 일반식으로 표시되는 화합물의 반응에 의한By the reaction of a compound represented by the following general formula [상기 식에서, R1,R2,R3,R0,측쇄에서로써 나타낸 탄소-탄소 결합, 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 이미 정의한 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.][Wherein, R 1 , R 2 , R 3 , R 0 , In the side chain The carbon-carbon bonds shown as and the carbon-carbon bonds between the 3- and 4-positions in the carbostyryl backbone are as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 하기 일반식으로 표시된 카르보스티릴 유도체의 제조방법.Method for producing a carbostyryl derivative represented by the following general formula. [상기 식에서, R1,R2,R3,R0,측쇄에서로써 나타낸 탄소-탄소 결합, 및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 이미 정의한 것과 같다; R4'은 할로겐원자, 페닐술포닐기(치환기로써 저급 알킬기를 가질 수 있는), 저급 알킬기 또는 페닐-저급 알킬기(치환기로써, 페닐고리에 할로겐원자를 가질 수 있는); 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.][Wherein, R 1 , R 2 , R 3 , R 0 , In the side chain The carbon-carbon bonds shown as and the carbon-carbon bonds between the 3- and 4-positions in the carbostyryl backbone are as defined above; R 4 ′ is a halogen atom, a phenylsulfonyl group (which may have a lower alkyl group as a substituent), a lower alkyl group or a phenyl-lower alkyl group (as a substituent, which may have a halogen atom in the phenyl ring); expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 5. 하기 일반식으로 표시되는 화합물과5. Compound represented by the following general formula (상기 식에서 R6,R7및 R8은 이미 정의하였다.)(Wherein R 6 , R 7 and R 8 are already defined.) 하기 일반식으로 표시되는 화합물의 반응에 의한By the reaction of a compound represented by the following general formula [상기 식에서, R1,R2,및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 이미 정의한 것과 같다; X는 할로겐원자이다; 식 의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.][Wherein, R 1 , R 2 , And the carbon-carbon bond between the 3- and 4-positions in the carbostyryl backbone is as defined above; X is a halogen atom; The substitution position of the side chain of the formula is either 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 하기 일반식으로 표시되는 카르보스티릴 유도체의 제조방법.Method for producing a carbostyryl derivative represented by the following general formula. [상기 식에서, R1,R2,R6,R7,R8,및 카르보스티릴 골격에서 3-과 4-위치 사이의 탄소-탄소 결합은 이미 정의한 것과 같다; 식의 측쇄의 치환 위치는 카르보스티릴 골격에서 3-,4-,5-,6-,7- 또는 8-위치 중 어느 하나이다.][Wherein, R 1 , R 2 , R 6 , R 7 , R 8 , And the carbon-carbon bond between the 3- and 4-positions in the carbostyryl backbone is as defined above; expression The substitution position of the side chain of is any of 3-, 4-, 5-, 6-, 7- or 8-position in the carbostyryl skeleton.] 6. 본 발명에 다른 카르보스티릴 유도체를 유효 성분으로써 함유함을 특징으로 하는 항-위궤양 치료에 이용되는 제약 조성물.6. A pharmaceutical composition for use in the treatment of anti-gastric ulcer, characterized by containing the carbostyryl derivative according to the present invention as an active ingredient. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019830003040A 1982-07-05 1983-07-04 Process for preparing carbostyril derivatives KR900006401B1 (en)

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JP57117312A JPS597169A (en) 1982-07-05 1982-07-05 Carbostyryl derivative
JP57117311A JPS597168A (en) 1982-07-05 1982-07-05 Carbostyryl derivative
JP117312/82 1982-07-05
JP117311/82 1982-07-05
JP117311 1985-05-28
JP117312 1985-05-28

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JPH01308258A (en) * 1989-04-27 1989-12-12 Otsuka Pharmaceut Co Ltd Carbostyril derivative
DE69207560T2 (en) * 1991-06-07 1996-06-27 Otsuka Pharma Co Ltd Antidiabetic
JP2872546B2 (en) * 1992-11-26 1999-03-17 大塚製薬株式会社 Intestinal mucosal damage protective agent
TWI340650B (en) 2004-01-21 2011-04-21 Otsuka Pharma Co Ltd Amine saly of carbostyril derivative
WO2013108644A1 (en) * 2012-01-20 2013-07-25 京都府公立大学法人 Rebamipide therapeutic agent for allergic conjunctivitis
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