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KR840007722A - 3-(5-아미노펜틸)-아미노-1-벤즈아제핀-2-온-1-알카노산의 제조방법 - Google Patents

3-(5-아미노펜틸)-아미노-1-벤즈아제핀-2-온-1-알카노산의 제조방법 Download PDF

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KR840007722A
KR840007722A KR1019840000630A KR840000630A KR840007722A KR 840007722 A KR840007722 A KR 840007722A KR 1019840000630 A KR1019840000630 A KR 1019840000630A KR 840000630 A KR840000630 A KR 840000630A KR 840007722 A KR840007722 A KR 840007722A
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더블유. 에이치. 왓티 제프리
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아놀드 자일러, 에른스트 알테르
시바 가이기 에이지
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Abstract

내용 없음.

Description

3-(5-아미노펜틸)-아미노-1-벤즈아제핀-2-온-1-알카노산의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. S-에난티오머로서 다음 일반식(II)의 화합물 또는 상술한 이성체를 함유한 입체이성체의 혼합물을 S-에난티오머로서 다음 일반식(III)의 화합물 또는 상술한 이성체를 함유한 혼합물과, 또는 다음 일반식(IV)의 화합물과, 잔기 R1, R2및 R3중 어느하나에 존재할 수 있는 일급아미노그룹 및/또는 하이드록시그룹을 일시적으로 보호하는 환원제 존재하에 알킬화시키거나, 또는 다음 일반식(V)의 학합물 또는 상술한 화합물을 함유한 입체 이성체의 혼압물을, 바람직하게는 반응물중의 어느 하나에서 아미노 및/또는 하이드록실 그룹을 일시적으로 보호하면서, 다음일반식(III B)의 화합물로 알킬화시키거나, 또는 다음 일반식(VI)의 화합물을 S-에난티오머로서 다음 일반식(VII)의 아민 또는 상술한 이성체를 함유한 혼합물로 환원제 존재하에 축합시키거나, 또는 다음 일반식(VII)의 화합물 또는 상술한 화합물을 함유한 입체이성체의 혼합물을 가용매분해시키거나, 또는 다음 일반식(IX)의 화합물 또는 상술한 화합물을 함유하는 입체 이성체의 혼합물 또는 그의 반응성 에스레르를 폐환시키거나, 또는 이중결합이 C3-C4, C4-C5및/또는 질소원자 및 인접한 탄소원자 사이의 측쇄에 위치하는 다음 일반식(X)의 화합물에서 하나 또는 두개의 이중결합을 환원제로 처리하여 포화시키거나, 또는 다음 일반식(XI)의 화합물 또는 상술한 화합물을 함유한 입체이성체의 혼합물에서 모노사이클릭락탐을 환개열시키거나, 또는 다음 일반식(XII)의 화합물 또는 상술한 화합물을 함유한 입체이성체의 혼합물을 가수소분해시키거나 또는 환원시키거나, 또는 다음 일반식(XIII)의 화합물 또는 상술한 화합물을 함유한 입체이성체의 혼합물을 다음 일반식(I)의 화합물로 전환시키거나, 또는 다음 일반식(XIV)의 화합물 또는 상술한 화합물을 함유한 이성체의 혼합물을 다음 일반식(I)의 화합물로 전환시키거나, 또는 Z1대지 Z2중 적어도 하나가 보호그룹이며 Z1대지 Z4의 나머지가 수소를 나타내는 다음 일반식(XV)의 화합물 또는 상술한 화합물을 함유한 입체이성체의 혼합물에서 보호그룹을 제거하여, R2및 R3중 하나 또는 둘이 하이드록시를 나타낼 수 있는 일반식(I)의 화합물을 수득하며;원한다면 생성된 일반식(I)의 화합물을 또다른 일반식(I)의 화합물로 전환시키고/시키거나, 원한다면 생성된 염-형성성질을 갖는 일반식(I)의 화합물을 그의 염으로 전환시키거나 또는 생성된 염을 그밖의 염으로 전환시기거나 또는 유리화합물을 이러한 염으로부터 유리시키고/시키거나, 원한다면 편광력(chirality)의 두중심에 대하여 특이한 s, s배위를 갖는 일반식(I)의 광학적 이성체를 일반식(I)의 화합물을 함유한 입체이성체형의 생성된 혼합물에서 분리시킴을 특징으로하여, 다음 일반식(I)의 3-(5-아미노펜틸)-아미노-1-벤즈아제핀-2-온-1-알카노산 및 그의 염을 제조하는 방법.
    상기식에서, R1은 4-아미노부틸을 나타내며, R2및 R3는 각각 서로 독립적으로, 하이드록시 또는 저급알콕시를 나타내고, S는 편광력을 나타대며, Z은 반응성 에스테르화된 하이드록실그룹이고, Y는 옥소, 수소와 함께 반응성 에스테르화되거나 에테르화된 하이드록실그룹 또는 2개의 반응성 에스테르화되거나 에테르화된 하이드록실 그룹 Z이며, 단, 상기 일반식(VII)에서, Y가 옥소 또는 비스-(에스테르화된 또는 에테르화된) 하이드록시인 경우 R1및 R2는 상술한 바와 같고, R0'및 R0''중 하나는 시아노이고, 나머지 하나는 시아노 또는 각각 상기에서 정의한 바와같은 COR2및 COR3이며, X는 옥소, 보호된 옥소, 또는 비스-(에스레르화되거나 에테르화된 하이드록시)를 나타대거나; 또는 X는 하나의 수소와 함께 하나의 하이드록시, 하나의 에스테르화되거나, 에테르화된 하이드록시를 나타내고, R4는 2-아미노에틸로 전환가능한 그룹이며, R5및 R6중 하나는 각각 상기에서 정의한 바와같은 COR2밋 COR3로 전환되는 그룹이며, 나머지 하나는 COR2또는 COR3이거나, 또는 R5및 R6둘다는 COR2및 COR3로 전환되는 그룹이고, 상기 일반식(XI)에서 R3는 하이드록시를 나타낸다.
  2. 제1항에 있어서, R1이 4-아미노부틸을 나타내고, R2및 R3는 각각 서로 독립적으로 하이드록시, 메톡시, 에톡시 또는 3급-부톡시를 나타나는 일반식(I)의 화합물 및 그의 염을 제조하는 방법.
  3. 제1항에 있어서, R1이 4-아미노부틸을 나타내고, R2는 하이드록시, 메톡시 또는 3급-부톡시를 나타내며, R3는 하이드록시 또는 에톡시를 나타대는 일반식(I)의 화합물 및 그의 염을 제조하는 방법.
  4. 제1항에 있어서, 3-[(5-아미노-1-카복시)-(1S)-펜틸아미노]-1-카복시메틸-2,3,4,5-테트라하이드로-1H-1-(3S)-벤즈아제핀-2-온 또는 그의 염을 제조하는 방법.
  5. 제1항에 있어서, 3-[(5-아미노-1-카복시)-(1S)-펜틸아미노]-1-카복시메틸-2,3,4,5-테트라하이드로-1H-1-(3S)-벤즈아제핀-2-온의 염산염 또는 이 염산염을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019840000630A 1983-02-10 1984-02-10 3-(5-아미노펜틸)-아미노-1-벤즈아제핀-2-온-1-알카노산 및 이의 염의 제조방법 KR900009023B1 (ko)

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US06/465,695 US4473575A (en) 1982-07-19 1983-02-10 3-Amino-(1)-benzazepin-2-one-1-alkanoic acids
US465695 1983-02-10

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KR840007722A true KR840007722A (ko) 1984-12-10
KR900009023B1 KR900009023B1 (ko) 1990-12-17

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FI77857C (fi) 1989-05-10
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EP0119954B1 (de) 1990-03-14
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AR242190A1 (es) 1993-03-31
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AR243163A1 (es) 1993-07-30
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GR79809B (ko) 1984-10-31
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ES8703859A1 (es) 1987-03-01
PT78075B (en) 1986-06-11
EP0119955B1 (de) 1989-12-13
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EP0119954A3 (en) 1986-06-11
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