KR830002744A - 구아니딘 화합물의 제조방법 - Google Patents
구아니딘 화합물의 제조방법 Download PDFInfo
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- C07D271/113—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
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Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (29)
- (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
- (b) 구조식(IV)의 구아니딘 화합물을 구조식(V)의 화합물과 반응시키거나, 또는
- (c) 구조식(VI)의 구아니딘 유도체 또는 이의토우토머형 유도체를 구조식(VII)의 화합물과 반응시키고
- (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
- (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
- (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.
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- 상기 구조식에서
- R1은 치환되거나 또는 비치환된 지방족 또는 싸이클로 지방족 탄화수소 래디칼이고, 또
- R2는 수소 또는 치환되거나 또는 비치환된 지방족 탄화수소 래디칼이거나, 또는
- R1및 R2가 함께 사슬중의 탄소원자가 이질성원자로 혼입될 수 있는 지방족 특성의 치환되거나 또는 비치환된 2가 탄화수소 래디칼이고,
- R3가 수소 또는 저급알킬이며,
- 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,
- 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
- Ph는 치환되거나 또는 비치환된 페닐래디칼이며,
- X1이 Ph가 치환되거나 또는 비치환된 페닐 래디칼 또는 분리가능기인 Ph-N=기이고,
- X2가 R 및 R2는 정기상의와 동일하거나 또는 분리가능기인기이며, 또
- X3는 R3,R4,R5및 Het가 C-N기와 결합하는 2가 헤테로알킬렌기로서 상기 정의와 같거나 또는 분리 가능기인
- 이고
- (단 X1,X2또는 X3치환체중 단 1개가 분리가능기이고 또 X1,X2또는 X3기중 1개가 탄소원자와 2중결합을 이룬다)
- Y는 메톡시 또는 에톡시등의 저급알콕시, 메틸 티오 또는 에틸티오등의 저급알킬티오, 또는 염소 또는 브롬등의 할로겐이거나 또는 Y는 동일 탄소원자에 위치한 2개의 저급알콕시기이며, 또
- 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)
- Y1은 옥소, 티옥소 또는 NH기이고 n1또는 n2가 모두 3이상이 아니라는 조건하에 0,1,2 또는 3이며,
- Z1은 할로겐원자이고, 또
- 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
- 을 만들며, 2가 래디칼 "알킬렌"은 사슬중 1개의 수소원자가 수소를 제외한 상기 R4의 정의와 동일한 치환체 R4'로치환된 3개 내지 5개 탄소원자의 알킬렌 사슬이고,
- R2'와 R3'치환체는 이중 1개는 상기 R2또는 R3의 정의와 동일하고 또 다른하나는 아미노보호기이거나 또는 R2및 R3가 모두 아미노보호기이다.
- ※참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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CH4995 | 1979-05-29 | ||
CH499579 | 1979-05-29 |
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KR830002744A true KR830002744A (ko) | 1983-05-30 |
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---|---|---|---|
KR1019800002110A KR830002744A (ko) | 1979-05-29 | 1980-05-28 | 구아니딘 화합물의 제조방법 |
Country Status (2)
Country | Link |
---|---|
US (1) | US4342764A (ko) |
KR (1) | KR830002744A (ko) |
Families Citing this family (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
-
1980
- 1980-05-19 US US06/151,031 patent/US4342764A/en not_active Expired - Lifetime
- 1980-05-28 KR KR1019800002110A patent/KR830002744A/ko unknown
Also Published As
Publication number | Publication date |
---|---|
US4342764A (en) | 1982-08-03 |
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