KR950701625A - 항발작 치료용 gaba 및 l-글루탐산 동족체(gbab and l-glutamic acid analogs for antiseizure treatment) - Google Patents

항발작 치료용 gaba 및 l-글루탐산 동족체(gbab and l-glutamic acid analogs for antiseizure treatment)

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KR950701625A
KR950701625A KR1019940704158A KR19940704158A KR950701625A KR 950701625 A KR950701625 A KR 950701625A KR 1019940704158 A KR1019940704158 A KR 1019940704158A KR 19940704158 A KR19940704158 A KR 19940704158A KR 950701625 A KR950701625 A KR 950701625A
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methyl
ester
phenyl
acid
azide
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리차드 비. 실버맨
리스자르트 안드루츠키에비치
포-와이 윤
데니스 마틴 소비에레이
로이드 찰스 프랭클린
마크 앤런 스츠윈드트
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인드라니 무크하르지
노스웨스턴 유니버시티
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Abstract

본 발명의 하기 일반식의 화합물에서,
R1은 1~6개의 탄소원자를 갖는 직쇄형 알킬기 또는 측쇄형 알킬기, 페닐, 또는 3~6개의 탄소원자를 갖는 시클로알킬이고; R2는 수소 또는 메틸이며; R3는 수소, 메틸 또는 카르복실이다.
이 화합물은 발작성 질병 치료에 유용하다.
또한 본 발명은 상기 화합물의 제조방법에 대해서도 기술하였다. 상기 화합물의 합성시 제조된 중간물질에 대해서도 기술하였다.

Description

항발작 치료용 GABA 및 L-글루탐산 동족체(GBAB AND L-GLUTAMIC ACID ANALOGS FOR ANTISEIZURE TREATMENT)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (16)

  1. 4-메틸-5-페닐-2-옥사졸리디논, 4-메틸-(2-메틸프로필)-2-디옥소-5-페닐-3-옥사졸리딘부탄산, 페닐메틸 에스테르, 4-메틸-펜타노일 클로라이드, 4-메틸-3-(4-메틸-1-옥소펜틸)-5-페닐-2-옥사졸리디논, 2-(2-메틸프로필)-부탄디산, 4-(페닐메틸)에스테르, 3-(아지도메틸)-5-메틸-헥산산, 페닐메틸 에스테르, 3-(히드록시메틸)-5-메틸-헥산산, 페닐메틸 에스테르, 5-메틸-3-[[[(4-메틸페닐)술포닐]옥시]-메틸]-헥산산, 페닐메틸 에스테르, 3-(아지도메틸)-5-메틸-헥산산, 2-(2-메틸프로필)-1,4-부틴디산, 4-(1,1-디메틸에틸)에스테르, 3-(아지도메틸)-5-메틸-1, 1-디메틸에틸에스테르, 3-(히드록시 메틸)-5-메틸-헥산산, 1, 1-디메틸에스테르, 5-메틸-3[[[(4-메틸(페닐)술포닐]옥시]-메틸-헥산산, 1,1-디메틸에틸에스테르, 또는 4-메틸-(2-메틸프필)-2-디옥소-5-페닐-3-옥사졸리딘부탄산, 1,1-디메틸에틸에스테르인 화합물.
  2. (S)-3-(아지도메틸)-5-메틸-헥산산인 화합물.
  3. (S)-3-(아지도메틸)-5-메틸-헥산산, 1,1-디메틸에틸에스테르인 화합물.
  4. (S)-5-메틸-3-[[[(4-메틸(페닐)술포닐]-옥시]메틸-헥산산, 1,1-디메틸에틸 에스테르, (S)-3-(히드록시메틸)-5-메틸-, 1,1-디-메틸에틸 에스테르, (S)-2-(2-메틸프로필)-1,4-부탄디산, 4-(1,1-디메틸에틸) 에스테르, 또는 (S)-4-메틸-(2-메틸프로필)-2-디옥소-5-페닐-3-옥사졸리딘부탄산, 1,1-디메틸에틸에스테르인 화합물.
  5. R1은 1~6개의 탄소원자를 갖는 직쇄형 알킬 또는 측쇄형 알킬, 페닐, 또는 3~6개의 탄소원자를 갖는 시클로알킬이고; R2가 수소 또는 메틸이며; R3가 수소, 메틸 또는 카르복실인 상기 일반식 Ⅰ의 비대칭 화합물의 제조 방법에 있어서, 다음 일반식의 아지드를 가수분해시켜
    다음 일반식의 중간물질 아지드를 만들고,
    중간물질 아지드를 환원시켜 다음 일반식의 아민을 제조함을 특징으로 하는 제조방법:
    위 식에서, R1과 R2는 제1항에 정의한 바와 같고, Ph는 페닐, Me는 메틸, Bn은 벤질을 나타낸다.
  6. 제5항에 있어서, 상기 아지드를 수산화나트륨으로 처리하여 가수분해 시킴을 특징으로 하는 제조방법.
  7. 제5항에 있어서, 상기 중간물질 아지드를 수성염기에서 추출하는 단계를 더 포함함을 특징으로 하는 제조방법.
  8. 제7항에 있어서, 상기 수성 추출물을 산성화시키는 단계를 더 포함함을 특징으로 하는 제조방법.
  9. 제5항에 있어서, 상기 중간물질 아지드를 중성 조건하에서 환원시켜 아미노산을 제공함을 특징으로 하는 제조방법.
  10. 제5항에 제조 방법으로 제조된 아미노산.
  11. Ⅰ
    R1은 1~6개의 탄소원자를 갖는 직쇄형 알킬이고; R2가 수소 또는 메틸이며; R3가 수소,메틸 또는 카르복실인 상기 일반식의 비대칭 화합물의 제조 방법에 있어서, 다음 일반식의 아지드를 가수분해시켜
    다음 일반식의 중간물질 아지드를 만들고,
    중간물질 아지드를 환원시켜 다음 일반식의 아민을 제조함을 특징으로 하는 제조방법:
    위 식에서, R1과 R2는 제1항에 정의한 바와 같고, ph는 페닐, Me는 메틸을 나타낸다.
  12. 제11항에 있어서, 상기 아지드를 수산화나트륨으로 처리하여 가수분해 시킴을 특징으로 하는 제조방법.
  13. 제11항에 있어서, 상기 중간물질 아지드를 수성염기에서 추출하는 단계를 더 포함함을 특징으로 하는 제조방법.
  14. 제13항에 있어서, 상기 수성 추출물을 산성화시키는 단계를 더 포함함을 특징으로 하는 제조방법.
  15. 제11항에 있어서, 상기 중간물질 아지드를 중성 조건하에서 환원시켜 아미노산을 제공함을 특징으로 하는 제조방법.
  16. 제11항의 제조 방법으로 제조된 아미노산.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940704158A 1992-05-20 1993-05-18 항발작 치료용 gaba 및 l-글루탐산 동족체(gbab and l-glutamic acid analogs for antiseizure treatment) KR950701625A (ko)

Applications Claiming Priority (3)

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US88608092A 1992-05-20 1992-05-20
US886,080 1992-05-20
PCT/US1993/004680 WO1993023383A1 (en) 1992-05-20 1993-05-18 Gaba and l-glutamic acid analogs for antiseizure treatment

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