KR860001791A - 질소함유 헤테로 사이클릭 화합물의 제법 - Google Patents

질소함유 헤테로 사이클릭 화합물의 제법 Download PDF

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KR860001791A
KR860001791A KR1019850005509A KR850005509A KR860001791A KR 860001791 A KR860001791 A KR 860001791A KR 1019850005509 A KR1019850005509 A KR 1019850005509A KR 850005509 A KR850005509 A KR 850005509A KR 860001791 A KR860001791 A KR 860001791A
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위톨드 프란츠만 카알
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더 웰컴 파운데이션 리미티드
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Abstract

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Description

질소함유 헤테로 사알클릭 화밥물의 제법
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Claims (3)

  1. 하기 일반식(ⅩⅢ)화합물을 고리화하거나 또는 R7이 수소, R8이 수소, C1-2알킬, 시아노 또는 니트로인 신규의 일반식(Ⅲ)와합물의 제조를 위하여, 하기 일반식(ⅩⅣ) 화합물을 하기 일반식(ⅩⅤ) 화합물과 축합시키거나 또는 R6a와 R6b가 모두 C1-4알킬기인 일반식(Ⅲ)의 신규화합물의 제조을 위하여는 하기 일반식(ⅩⅥ) 화합물을 하기 일반식(ⅩⅦ) 화합물과 반응시키며 R6b가 기 CH2R6 c이며 R6 c가 수도 또는 C1-3알킬인 일반식(Ⅲ)의 신규화합물의 제조를 위하여는 하기 일반식(ⅩⅥa) 화합물을 일반식(ⅩⅦ) 화합물과 반응시키거나 또는 하기 일반식(ⅩⅧ) 화합물을 고리화하여 일반식(Ⅲ)의 한가지 신규화합물을 일반식(Ⅲ)의 다른 신규화합물로 전환시키는 것을 특징으로 하는 일반식(Ⅲ)화합물의 제조방법.
    (상기식(Ⅲ)에서 점선은 단일결합 또는 이중결합을 표시하며; 그 점선이 이중결합일때 m은 0이며 그점선이 단일결합일때 m은 1이고; R0는 수소 또는 CH2R10; R1은 수소 또는 브롬, 염소, 메톡시, 메틸, 트리플루오로메틸 또는 메틸티오로부터 선택된 치환분이며;R2,R3와 R4는 동일하거나 상이하게 각각 수소 또는 식 R10-A-의 기로 이때 R10은 수소 또는 할로겐, 플루오로설포닐, 시아노, 하이드록시, 티오, 니트로, C1-3알콕시 또는 C1-3알킬티오로 임의로 치한된 C1-16하이드로 카르빌로 이때 알콕시와 알킬이오기는 다시 임의로 할로겐, 하이드록시, 티오, C1-2알콕시 또는 C1-2알킬티오로 치환되며 A는 산소, 황 또는 메틸렌이다; 또는 R1-R4의 어떠한 두개의 인접 치환분은 함께 메틸렌 디옥시 또는 에틸렌디옥시기를 형성한다; R5a는 수소 또는 C1-12아하이드로카르빌이며, R5b는 수소 또는 R5a와 R5b는 각각 C1-4알킬 또는 R5a와 R5b는 그들과 결합된 탄소원자와 함께 C3-8스피로 사이클로알킬고리를 형성한다;
    R6a와 R6b는 동일하거나 상이하며 각각 수소 또는 C1-12하이드로카르빌 또는 그들과 결합된 탄소원자와 함께, C3-8스피로사이클로알킬고리를 형성한다; 또는 R5a와 R6a는 그들과 결합된 탄소원자와 함께, 임의로 2개까지의 이중결합을 포함하는 5 내지 6탄소의 카르보사이클릭 환을 형성한다; R7은 수소 또는 불소; R8은 수소, 할로겐, 시아노, 니트로 또는 하나이상의 할로겐 원자로 임의 치한된 C1-2알킬; R9는 -(CH=CH)nR11로 n은 0-2이며 R11은 수소, C1-8알킬, C2-8알케닐, C2-8알키닐, 또는 3개 내지 16탄소를 함유하며 하이드록시, 티오, 할로겐, 플루오로설포닐, 니트로, 시아노, C1-12하이드로카르빌, C1-12하이드로카르빌옥시, C1-12하이드로카르빌티오로임의 치환된 모노사이클릭, 비이사이클릭, 트리사이클릭 또는 테트라사이클릭환으로 상기의 하이드로카르빌, 하이드로 카르빌옥시와 하이드로카르빌티오기는 각각 다시 할로겐하이드록시, 티오 C1-2알킬티오 또는 C1-2알콕시기로 임의 치한된다;
    R8과 R9는 임의로 C1-4알킬렌 다리를 거쳐 결합된다; 상기식(ⅩⅢ)에서; R1-R7은 전술한 바와같고 Z1은 수소이며 X1-C-Y1은 C=O기, 또는 X1이 이탈기이며 Y1과 Z1은 함께 Ca와 N사이에서 이중결합을 형성; 상기식(ⅩⅣ)에서 R1-R6이 전술한 바와같고 R8a와 R8b가 모두 수소이거나 함께기=R(O알킬)2또는 =PPh′3를 형성; 상기식(ⅩⅤ)에서 R7과 R9는 전술한 바와 같음; 상기식(ⅩⅥ)과 (ⅩⅦ)에서 R1-R5와 R7-R9는 전술한 바와 같고 R6a와 R6b가 동일 또는 상이하며 각각 C1-4알킬기 X2가 이탈기임; 상기식(ⅩⅥa)과 (ⅩⅦ)에서 R1-R9는 전술한 바와 같다).
  2. 일반식(Ⅲ)화합물을 하나이상의 약학적 허용담체 또는 부형제와 함께 함유하는 약학제형.
    (여기에서, 점선은 단일결합 또는 이중결합을 표시하며; 그 점선이 이중결합일때 m은 0이며 그 점선이 단일결합일때 m은 1이다; R10은 수소 또는 CH2R10; R1은 수소 또는 브롬, 염소, 메톡시, 메틸, 트리플루오로메틸 또는 메틸티오로부터 선택된 치환분이며; R2,R3와 R4는 동일하거나 상이하게 각각 수소 또는 식 R10-A-의 기로 이때 R10은 수소 또는 할로겐, 플루오로설포닐, 시아노, 하이드록시, 티오, 니트로, C1-3알콕시 또는 C1-3알킬티오로 임의로 치한된 C1-16하이드로 카르빌로 이때 알콕시와 알킬이오기는 다시 임의로 할로겐, 하이드록시, 티오, C1-2알콕시 또는 C1-2알킬티오로, 치환되며 A는 산소, 황 또는 메틸렌이다; 또는 R1-R4의 어떠한 두개의 인접치환분은 함께 메틸렌 디옥시 또는 에틸렌디옥시기를 형성한다; R5a는 수소 또는 C1-12아하이드로카르빌이며, R5b는 수소 또는 R5a와 R5b는 각각 C1-4알킬 또는 R5a와 R5b는 그들과 결합된 탄소원자와 함께 C3-8스피로 사이클로알킬고리를 형성한다;
    R6a와 R6b는 동일하거나 상이하며 각각 소소 또는 C1-12하이드로카르빌 또는 그들과 결합된 탄소원자와 함께, C3-8스피로사이클로알킬 고리를 형성한다; 또는 R5a와 R6a는 그들과 결합된 탄소원자와 함께, 임의로 2개까지의 이중결합을 포함하는 5 내지 6탄소의 카르보사이클릭 환을 형성한다; R7은 수소 또는 불소; R8은 수소, 할로겐, 시아노, 니트로 또는 하나이상의 할로겐 원자로 임의 치한된 C1-2알킬; R9은 -(CH=CH)nR11로 n은 0-2이며 R11은 수소, C1-8알킬, C2-8알케닐, C2-8알키닐, 또는 3 내지 16탄소를 함유하며 하이드록시, 티오, 할로겐, 플루오로설포닐, 니트로, 시아노, C1-12하이드로카르빌, R1-12하이드로카르빌옥시, C1-12하이드로카르빌티오로 임의 치환된 모노사이클릭, 비이사이클릭, 트리사이클릭 또는 테트라사이클릭환으로 상기의 하이드로카르빌, 하이드로카르빌옥시와 하이드로카르빌티오 각각 다시 할로겐, 하이드록시, 티오 C1-2알킬티오 또는 C1-2알콕시기로 임의 치한된다;
    R8과 R9는 임의로 C1-4알킬렌 다리를 거쳐 결합된다;
  3. 제2항에 있어서, 국소투여를 위한 제형.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019850005509A 1984-08-01 1985-07-31 질소함유 헤테로시클릭 화합물의 제조방법 KR920004484B1 (ko)

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GB848419658A GB8419658D0 (en) 1984-08-01 1984-08-01 Nitrogen containing heterocyclic compounds
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PL352041A1 (en) * 1999-07-29 2003-07-28 Derivatives of isochynoline, pharmaceutical compositions containing these derivatives and method of obtaining an active substance
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US20030149038A1 (en) * 2001-11-09 2003-08-07 The Regents Of The University Of California Alpha-helix mimicry by a class of organic molecules
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