KR830002744A - 구아니딘 화합물의 제조방법 - Google Patents

구아니딘 화합물의 제조방법 Download PDF

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KR830002744A
KR830002744A KR1019800002110A KR800002110A KR830002744A KR 830002744 A KR830002744 A KR 830002744A KR 1019800002110 A KR1019800002110 A KR 1019800002110A KR 800002110 A KR800002110 A KR 800002110A KR 830002744 A KR830002744 A KR 830002744A
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지. 데이브 크리스나
죠지 토마스
아이. 비스와나탄 나라야나
일베스파 애초
프라이 죠르그
쉬바이져 에른스트
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아놀드 세일러 및 애른스트 알트헤르
시바가이기 에이지
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Abstract

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Description

구아니딘 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (29)

  1. (a) 구조식(II)의 화합물을 분리가능기(Detachable group)로 치환시키기 위해서 다음 X1,X2또는 X3에서 정의한 결핍아미노 또는 이미노기와 동일한 아민 또는 이민과 반응시키거나, 또는
  2. (b) 구조식(IV)의 구아니딘 화합물을 구조식(V)의 화합물과 반응시키거나, 또는
  3. (c) 구조식(VI)의 구아니딘 유도체 또는 이의토우토머형 유도체를 구조식(VII)의 화합물과 반응시키고
  4. (d) Het가 C-N기와 함께 6개 내지 8개 구성원 헤테로싸이클 고리를 이룰수 있는 사슬에 4개 내지 6개구성원을 갖는 헤테로알킬렌 래디칼인 구조식(I)의 화합물을 제조하는데 있어, 구조식(VI)의 화합물을 구조식(VIII)의 할로겐알킬렌 이소티오시아네이트와 반응시키거나 또는
  5. (e) R1이 다음 정의와 동일하고 또 R2와 R3가 수소인 구조식(I)의 화합물을 제조하는데 있어, R2와 R3가 수소가 아니고 다음의 R2와 R3의 정의와 동일한 구조식(I)의 화합물을 지방족 또는 싸이클로 지방족 알콜의 반응 에스테르와 같은 알킬화제와 반응시키거나, 또는
  6. (f) 구조식(IX)의 화합물을 분리하거나 또 필요한 경우 다른 방법으로 처리하고 또 필요한 경우 수득한 구조식(I)의 화합물을 염으로 바꾸고 또 필요한 경우 수득한 구조식(I)화합물의 염을 유리염기로 바꾸는 것을 특징으로 하는 구조식(I)의 구아니딘 유도체 및 이의 토우토머화합물과 그염의 제조방법.
  7. 상기 구조식에서
  8. R1은 치환되거나 또는 비치환된 지방족 또는 싸이클로 지방족 탄화수소 래디칼이고, 또
  9. R2는 수소 또는 치환되거나 또는 비치환된 지방족 탄화수소 래디칼이거나, 또는
  10. R1및 R2가 함께 사슬중의 탄소원자가 이질성원자로 혼입될 수 있는 지방족 특성의 치환되거나 또는 비치환된 2가 탄화수소 래디칼이고,
  11. R3가 수소 또는 저급알킬이며,
  12. R4가 수소, 저급알킬, 저급알콕시, 저급알킬티오, 저급알킬아미노, 2-저급알킬아미노, 할로겐, 저급알콕시카보닐, 트리플루오로메틸 또는 치환되거나 또는 비치환된 페닐 또는 양측으로 1결합수와 옥소기를 갖는 탄소원자이고 R5는 수소 또는 저급알킬이며,
  13. Het가 C-N기와 함께 고리에 산소, 유황 또는 질소등으로 구성되는 군으로부터 선정한 2개 내지 3개의 이성질원자를 갖는 5구성원헤테로 싸이클고리를 이루고, 불포화일 수 있는 3개 사슬 구성원의 헤테로알킬렌 래디칼이거나 또는 Het 가 C-N기와 함께 질소이외에 산소, 유황 또는 질소등의 군으로 부터 선정한 기타 이질성원자를 함유하는 6개 내지 8개 구성원 헤테로싸이클 고리를 이루는 사슬에 4개 내지 6개 구성원을 갖는 헤테로알킬렌래디칼이고, 또
  14. Ph는 치환되거나 또는 비치환된 페닐래디칼이며,
  15. X1이 Ph가 치환되거나 또는 비치환된 페닐 래디칼 또는 분리가능기인 Ph-N=기이고,
  16. X2가 R 및 R2는 정기상의와 동일하거나 또는 분리가능기인기이며, 또
  17. X3는 R3,R4,R5및 Het가 C-N기와 결합하는 2가 헤테로알킬렌기로서 상기 정의와 같거나 또는 분리 가능기인
  18. 이고
  19. (단 X1,X2또는 X3치환체중 단 1개가 분리가능기이고 또 X1,X2또는 X3기중 1개가 탄소원자와 2중결합을 이룬다)
  20. Y는 메톡시 또는 에톡시등의 저급알콕시, 메틸 티오 또는 에틸티오등의 저급알킬티오, 또는 염소 또는 브롬등의 할로겐이거나 또는 Y는 동일 탄소원자에 위치한 2개의 저급알콕시기이며, 또
  21. Z는 테트라플루오로보레이트 음이온, 플루오로 설폰에이트음이온, 메탄설폰에이트음이온등의 알칸설폰에이트음이온, 또는 염소 또는 브롬등의 할라이드이고, (Y가 동일 탄소원자에 위치한 2개의 저급알콕시인 경우 Z음이온은 없거나 또는 R3가 수소인 경우 토우토머형 유도체는 유리염기로서 존재한다)
  22. Y1은 옥소, 티옥소 또는 NH기이고 n1또는 n2가 모두 3이상이 아니라는 조건하에 0,1,2 또는 3이며,
  23. Z1은 할로겐원자이고, 또
  24. Z2는 옥소기 또는 수소원자가 메틸렌기의 일부인 경우 수소 및 할로겐으로서 구성되는 기이거나 또는 n1또는 n2가 모두 0인 경우 Z1및 Z2가 함께 이미노기를 통하여 R4및 R5가 수소인 아리지딘 유도체를 이루는 2가 알킬렌 래디칼
  25. 을 만들며, 2가 래디칼 "알킬렌"은 사슬중 1개의 수소원자가 수소를 제외한 상기 R4의 정의와 동일한 치환체 R4'로치환된 3개 내지 5개 탄소원자의 알킬렌 사슬이고,
  26. R2'와 R3'치환체는 이중 1개는 상기 R2또는 R3의 정의와 동일하고 또 다른하나는 아미노보호기이거나 또는 R2및 R3가 모두 아미노보호기이다.
  27. ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019800002110A 1979-05-29 1980-05-28 구아니딘 화합물의 제조방법 KR830002744A (ko)

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US5188840A (en) * 1985-09-26 1993-02-23 Chugai Seiyaku Kabushiki Kaisha Slow-release pharmaceutical agent
GB8903592D0 (en) * 1989-02-16 1989-04-05 Boots Co Plc Therapeutic agents
US7008979B2 (en) 2002-04-30 2006-03-07 Hydromer, Inc. Coating composition for multiple hydrophilic applications
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
US20080312435A1 (en) * 2004-11-15 2008-12-18 Taisho Pharmaceutical Co., Ltd. Imine Compound
CN106749078B (zh) * 2015-11-23 2019-01-04 中国科学院大连化学物理研究所 一种2-亚胺基恶唑的合成方法

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US2762815A (en) * 1955-04-06 1956-09-11 Commercial Solvents Corp 3-isoxazolidones, derivatives and process
AU5263779A (en) * 1978-11-29 1980-05-29 Beecham Group Limited Derivatives of thiazolidin-2-ylidene and oxazolidin-2-ylidene with hypoglycaemic acitivity

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