KR830002757A - 피리미딘 화합물의 제조방법 - Google Patents

피리미딘 화합물의 제조방법 Download PDF

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Publication number
KR830002757A
KR830002757A KR1019800001944A KR800001944A KR830002757A KR 830002757 A KR830002757 A KR 830002757A KR 1019800001944 A KR1019800001944 A KR 1019800001944A KR 800001944 A KR800001944 A KR 800001944A KR 830002757 A KR830002757 A KR 830002757A
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South Korea
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compound
formula
salt
halogen
group
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KR1019800001944A
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English (en)
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막서 아드리안
아이헨베르거 쿠르트
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아놀드 자일러, 에른스트 알테르
시바-가이기 에이지
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Publication of KR830002757A publication Critical patent/KR830002757A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms

Abstract

내용 없음

Description

피리미딘 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. 구조식 Py-X(Ⅳ)화합물 또는 그 염과 다음 구조식(Ⅵ)화합물 또는 그 염을 반응시키거나, 다음 구조식(Ⅶ)화합물 또는 상응하는 호변이성체형 또는 그 염을 구조식 H2N-Alk-NHR1(Ⅷ)의 알킬렌디아민 화합물과 반응시키거나, 다음 구조식(XII)의 포스핀산 할로겐화물을 구조식 Py-NH-R2(Ⅳa)의 아민 화합물과 반응시키고, 필요하면, Py에 할로겐이 함유된 구조식(Ⅰ)화합물을 탈할로겐화하거나, Py가 2-및 6-위치에서 할로겐으로 치환된 생성 화합물에서 2-위치의 할로겐을 치치환 또는 치환아미노로대치하고/또는 어떤 생성화합물을 본 발명의 다른 화합물로 전환하고/또는 필요하면 생성염기를 그것의 산부가염으로 또는 생성된 염을 상응하는 유리염기 또는 산부가염으로 전환하고/또는, 필요하면 수득한 이성청 혼합물을 단일이 성체로 분해하여 다음 구조식(Ⅰ)의 신규 2-(피리미디닐아미노)-1, 3-디아지-2-사이클로알켄 화합물, 그들의 호변이성체 화합물 및 산부가염을 제조하는 방법.
  4. 상기 식에서 Py는 탄소원자에 의해 질소원자에 결합된 임의 치환된 4-또는 5-피리미디닐 라디칼이고, R1및 R2는 각각 수소, 저급 알킬 또는 저급알케닐이고, Alk는 두 질소원자를 가르는 탄소수 2 내지 4의 저급알킬렌이고, 라디칼 X 및 Y 중 하나는 구조식 -N(R2)-H(Ⅵ)의 아미노그룹이고 나머지는 반응조건 하에서 수소와 함께 분리될 수 있는 그룹이고, Y1은 분리될 수 있는 아미노그룹, 옥소-또는 티옥소그룹이고, Y2는 분리될 수 있는 그룹이거나, R2가 수소이면 Y1및 Y2함께 삼중결합 질소원자이고, Hal은 할로겐이다.
  5. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019800001944A 1979-05-18 1980-05-17 피리미딘 화합물의 제조방법 KR830002757A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH466979 1979-05-18
CH4669 1979-05-18

Publications (1)

Publication Number Publication Date
KR830002757A true KR830002757A (ko) 1983-05-30

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KR1019800001944A KR830002757A (ko) 1979-05-18 1980-05-17 피리미딘 화합물의 제조방법

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Country Link
EP (1) EP0019811A1 (ko)
JP (1) JPS55154971A (ko)
KR (1) KR830002757A (ko)
AR (1) AR228256A1 (ko)
AU (1) AU5848480A (ko)
DD (1) DD150609A5 (ko)
DK (1) DK214480A (ko)
ES (1) ES491514A0 (ko)
FI (1) FI801600A (ko)
GB (1) GB2052487B (ko)
GR (1) GR68453B (ko)
IE (1) IE49803B1 (ko)
IL (1) IL60086A (ko)
MA (1) MA18829A1 (ko)
NO (1) NO801469L (ko)
NZ (1) NZ193730A (ko)
OA (1) OA06533A (ko)
PL (1) PL224313A1 (ko)
PT (1) PT71251A (ko)
ZA (1) ZA802909B (ko)
ZW (1) ZW11880A1 (ko)

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US4507146A (en) * 1982-12-28 1985-03-26 Ciba-Geigy Corporation 2,4-Diamino-6-halo-5-trifluoromethylpyrimidines having herbicidal activity
DE3829469A1 (de) * 1988-08-31 1990-03-01 Bayer Ag Verfahren zur herstellung von substituierten n-azinyl-n'-sulfonyl-isothioharnstoffen und n-azinyl-iminodithiokohlensaeure-s,s-diester als zwischenprodukte zu ihrer herstellung
EP0954316A4 (en) * 1997-09-03 2002-02-13 Lilly Co Eli PYRIMIDINE DERIVATIVES
CA2422371C (en) 2000-09-15 2010-05-18 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20030105090A1 (en) 2000-12-21 2003-06-05 David Bebbington Pyrazole compounds useful as protein kinase inhibitors
CZ20032341A3 (cs) * 2001-01-31 2004-12-15 Synaptic Pharmaceutical Corporation Použití antagonistů GAL3 receptoru pro léčbu deprese a/nebo úzkosti
KR20040099324A (ko) 2002-03-13 2004-11-26 유로-셀티큐 에스.에이. 아릴 치환된 피리미딘 및 이것의 용도
US20040009981A1 (en) 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
WO2003077656A1 (en) * 2002-03-15 2003-09-25 Ciba Specialty Chemicals Holding Inc. 4-aminopyrimidines and their use for the antimicrobial treatment of surfaces
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
CN101037438A (zh) 2002-08-02 2007-09-19 沃泰克斯药物股份有限公司 用作gsk－3的抑制剂的吡唑组合物
US7601718B2 (en) 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
ATE542814T1 (de) 2005-08-18 2012-02-15 Vertex Pharma Pyrazinkinaseinhibitoren
BRPI0619708A2 (pt) 2005-11-03 2011-10-11 Vertex Pharma composto, composição, método para inibir a atividade da proteìna aurora quinase numa amostra biológica, método para tratar distúrbio proliferativo e método para tratar cáncer
AU2007317435A1 (en) 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
NZ577768A (en) 2006-12-19 2012-01-12 Vertex Pharma Aminopyrimidines useful as inhibitors of protein kinases
ES2435997T3 (es) 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopirimidinas útiles como inhibidores de las proteínas cinasas
JP5393489B2 (ja) 2007-03-09 2014-01-22 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリミジン
JP2010520887A (ja) 2007-03-09 2010-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリジン
JP2010523700A (ja) 2007-04-13 2010-07-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼインヒビターとして有用なアミノピリミジン
MX2009011810A (es) 2007-05-02 2010-01-14 Vertex Pharma Tiazoles y pirazoles utiles como inhibidores de cinasa.
WO2008137621A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AR067762A1 (es) 2007-07-31 2009-10-21 Vertex Pharma Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma
WO2010027921A1 (en) 2008-09-03 2010-03-11 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical formulations comprising the same
EP2364314B1 (en) * 2008-12-09 2014-03-12 Gilead Sciences, Inc. Modulators of toll-like receptors
KR102328682B1 (ko) * 2018-08-27 2021-11-18 주식회사 대웅제약 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물

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Also Published As

Publication number Publication date
AU5848480A (en) 1980-11-20
AR228256A1 (es) 1983-02-15
PL224313A1 (ko) 1981-02-13
ZA802909B (en) 1981-05-27
ZW11880A1 (en) 1980-12-17
JPS55154971A (en) 1980-12-02
PT71251A (en) 1980-06-01
GB2052487A (en) 1981-01-28
DD150609A5 (de) 1981-09-09
GR68453B (ko) 1981-12-30
FI801600A (fi) 1980-11-19
DK214480A (da) 1980-11-19
ES8104279A1 (es) 1981-04-16
IE801023L (en) 1980-11-18
NZ193730A (en) 1982-12-21
EP0019811A1 (de) 1980-12-10
IE49803B1 (en) 1985-12-25
OA06533A (fr) 1981-07-31
IL60086A0 (en) 1980-07-31
GB2052487B (en) 1983-05-11
MA18829A1 (fr) 1980-12-31
IL60086A (en) 1984-03-30
ES491514A0 (es) 1981-04-16
NO801469L (no) 1980-11-19

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