KR830003466A - 1-benzocepin-5 (2H) -one derivatives and methods for preparing these salts - Google Patents

1-benzocepin-5 (2H) -one derivatives and methods for preparing these salts Download PDF

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KR830003466A
KR830003466A KR1019800003006A KR800003006A KR830003466A KR 830003466 A KR830003466 A KR 830003466A KR 1019800003006 A KR1019800003006 A KR 1019800003006A KR 800003006 A KR800003006 A KR 800003006A KR 830003466 A KR830003466 A KR 830003466A
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South Korea
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group
hydrogen atom
alkyl
formula
acid addition
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KR1019800003006A
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Korean (ko)
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오렌도르프 헨리히-빌헤름
볼프 크라우스-울리흐
카우프만 빌헬름
하이네만 헨닝
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한스 에이취·스텐더, 닥터 베르네르 헨니에스
칼리-케미 파마 쥐엠비 에이취
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Priority to KR1019800003006A priority Critical patent/KR830003466A/en
Publication of KR830003466A publication Critical patent/KR830003466A/en

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Abstract

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Description

1-벤조세핀-5(2H)-온 유도체류와 이들염류의 제조방법.1-benzosepin-5 (2H) -one derivatives and methods for preparing these salts.

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

Claims (4)

다음 구조식(Ⅱ)화합물인 언급한 유도체의 산부가염류 또는 다음 구조식(Ⅳ)화합물을 다음 구조식(Ⅲ)화합물의 아민과 본활성용매에서 반응시켜 다음 구조식(Ⅰ)의 A/3-아미노-1-벤조세핀-5(2H)-온 유도체와 이들의 산부가염류의 제조방법.The acid addition salts of the above-mentioned derivatives of the following formula (II) or the following formula (IV) are reacted with the amine of the following formula (III) in the present active solvent and then A / 3-amino-1 of the following formula (I) -Benzosepin-5 (2H) -one derivatives and their acid addition salts. 상기 구조식에서In the above structural formula R1과 R2는 각기 수소원자, 치환되지 않은 페닐기로 임의로 말단 치환된 C1-C5-알킬기 또는 하나 또는 두 할로겐원자 또는 메틸 또는 메톡시기 또는 3,4-메틸렌디옥시 또는 3,4-메틸렌디옥시기로 치환된 페닐기, 하이드록실 그룹 또는 메톡시기로 임의로 말단 치환된 C2-C5-알킬 또는 C3-C4-알켄일기, 또는 R1과 R2중 하나는 수소원자 또는 C1-C5-알킬기이고 다른 것을 -NR5R6기로 말단치환된 C2-C5-알킬기, 상기에서 R5와 R6는 각기 수소원자 또는 C1-C5-알킬기, 또는 R5와 R6는 다른 하나에 직접 또는 산소, 황과질소로부터 선택된 헤테로원자를 경유하여 연결되어 질소원자를 포함하는 5-각 내지 7-각링을 형성하거나 또는 R1와 R2는 다른 하나에 직접 연결되거나 또는 산소, 황과 질소-R7으로부터 선택된 헤테로원자를 경유하여 연결된 알킬렌 기일수 있으며 질소원자를 포함하는 5-각 내지 7-각 링을 형성하며 상기에서 R7을 수소원자 또는 메틸-벤질 또는 페닐기 : R3와 R4는 각기 수소원자·할로겐원자 또는 C1-C4-알킬, C1-C4-알콕시 또는 C1-C4-알킬티오기, 또는 R3과 R4중 하나는 트리플루오로메틸그룹 또는 니트로그룹이고 다른 것은 수소원자 : 이고 X는 염소 또는 취소원자이다.R 1 and R 2 are each a hydrogen atom, a C 1 -C 5 -alkyl group optionally substituted with an unsubstituted phenyl group or one or two halogen atoms or a methyl or methoxy group or 3,4-methylenedioxy or 3,4- A C 2 -C 5 -alkyl or C 3 -C 4 -alkenyl group optionally terminated with a phenyl group, a hydroxyl group or a methoxy group substituted with a methylenedioxy group, or one of R 1 and R 2 is a hydrogen atom or C 1 -C 5 - alkyl group and the other is -NR 5 R 6 group to the terminal-substituted C 2 -C 5 - alkyl group, at the R 5 and R 6 are each a hydrogen atom or a C 1 -C 5 - alkyl group, or R 5 and R 6 is directly connected to the other or via a heteroatom selected from oxygen, sulfur and nitrogen to form a 5-angle to 7-angle ring containing nitrogen atoms, or R 1 and R 2 are directly connected to the other or Alkyl linked via a heteroatom selected from oxygen, sulfur and nitrogen-R 7 It may be a ethylene group and forms a 5-angle to 7-angle ring containing a nitrogen atom, wherein R 7 is a hydrogen atom or a methyl-benzyl or phenyl group: R 3 and R 4 are each a hydrogen atom, a halogen atom or a C 1 -group. C 4 -alkyl, C 1 -C 4 -alkoxy or C 1 -C 4 -alkylthio group, or one of R 3 and R 4 is a trifluoromethyl group or nitro group and the other is a hydrogen atom: and X is chlorine Or a cancellation atom. 구조식(Ⅰ)의 유도체를 유리 염기로 연속적으로 전환되는 산부가염 형태로 회수시키는 청구범위 1에서 청구된 공정.The process as claimed in claim 1, wherein the derivative of formula (I) is recovered in the form of an acid addition salt which is continuously converted to the free base. 구조식(Ⅰ)의 유도체를 무기 또는 유기산과 반응에 의해 산부가염으로 연속적으로 전환되는 유리염기형태로 회수되는 청구범위 1에서 청구된 공정.The process as claimed in claim 1, wherein the derivative of formula (I) is recovered in the form of a free base which is subsequently converted to an acid addition salt by reaction with an inorganic or organic acid. 다음 구조식(Ⅴ)화합물을 리듐하이드리드, 소디움하이드리드와 리듐-3급-부틸레이트로부터 선택된 강염기와 -70°C내지 용매의 비점 온도에서 불활성용매의 존재하에 반응시켜 다음구조식(Ⅱ)의 2,3,4,5-테트라하이드로-1-벤조세핀-3,5-디온유도체를 제조하는 방법.The compound of formula (V) is reacted in the presence of an inert solvent at a boiling point temperature of -70 ° C. to a solvent with a strong base selected from lithium hydride, sodium hydride and lithium tert-butylate. A method for producing a 3,4,5-tetrahydro-1-benzocepin-3,5-dione derivative. 상기 구조식에In the above structural formula R3과 R4는 청구범위 1에서 정의한 것이고 R8은 직쇄 또는 촉쇄 C1-C6알킬기이다.R 3 and R 4 are defined in claim 1 and R 8 is a straight or cyclic C 1 -C 6 alkyl group. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019800003006A 1980-07-28 1980-07-28 1-benzocepin-5 (2H) -one derivatives and methods for preparing these salts KR830003466A (en)

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KR1019800003006A KR830003466A (en) 1980-07-28 1980-07-28 1-benzocepin-5 (2H) -one derivatives and methods for preparing these salts

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