KR910018375A - N-[3-(1h-이미다졸-1-일)페닐]-4-(치환된)-2-피리미디나민 합성을 위한 개선된 방법 - Google Patents

N-[3-(1h-이미다졸-1-일)페닐]-4-(치환된)-2-피리미디나민 합성을 위한 개선된 방법 Download PDF

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KR910018375A
KR910018375A KR1019910006612A KR910006612A KR910018375A KR 910018375 A KR910018375 A KR 910018375A KR 1019910006612 A KR1019910006612 A KR 1019910006612A KR 910006612 A KR910006612 A KR 910006612A KR 910018375 A KR910018375 A KR 910018375A
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South Korea
Prior art keywords
imidazol
phenyl
substituted
pyridinyl
pyrimidinamine
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KR1019910006612A
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KR0168679B1 (ko
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데니스 디인 윌리엄
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알퐁스 아아르 노에
아메리칸 사이아나밋드 캄파니
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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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Photoreceptors In Electrophotography (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)

Abstract

내용 없음

Description

N-[3-(1H-이미다졸-1-일)페닐]-4-(치환된)-2-피리미디나민 합성을 위한 개선된 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 (a), (b)단계로 구성되는 치환체가 2-피리디닐, 3-피리디닐, 4-피리디닐, 2-푸라닐 및 2-티에닐로 구성된 기로부터 선택되는N-〔3-(1H-이미다졸-1-일)페닐〕-4-(치환된)-2-피리미디나민을 제조하는 방법, (A) 반응 pH를 약 pH2-3.5로 조절하면서, 3-(1H-이미다졸-1-일)벤즈아민을 시아나미드 및 할로겐산과 반응시키고 나서 〔3-(1H-이미다졸-1-일)페닐〕구아니딘, 디히드로콜로라이드를 회수하는 단계 ; 및 (B) (A)에서 회수된 〔3-(1H-이미다졸-1-일)페닐〕구아니딘, 디히드로클로라이드와 3-디메틸아미노-1(치환된)-2-프로펜-1-온 및 적당한 용매내 염기를 약 pH 10.5∼11.5에서 반응시켜서, -N-〔3-(1H-아미다졸-1-일)페닐〕-4-(치환된)-2-프리미디나민을 회수하는 단계.
  2. 제1항에 있어서, 상기 할로겐 산이 브롬화수소, 또는 염화 수소롤 구성되는 방법.
  3. 제2항에 있어서, 상기 할로겐 산이 가스 염화수소로 구성되는 방법.
  4. 제1항에 있어서, 상기 염기가 10N NaOH로 구성되는 방법.
  5. 제1항에 있어서, 상기 〔3-(1H-이미다졸-1-일)페닐〕구아니딘, 디히드로클로라이드가 여과에 의해 회수되는 방법.
  6. 제1항에 있어서, N-〔3-(1H-이미다졸-1-일)페닐〕-4-(2-피리디닐)-2-피리미디나민에 제조되는 방법.
  7. 제1항에 있어서, N-〔3-(1H-이미다졸-1-일)페닐〕-4-(3-피리디닐)-2-피리미다니민이 제조되는 방법.
  8. 제1항에 있어서, N-〔3-(1H-이미다졸-1-일)페닐〕-4-(4-피리디닐)-2-피리미디나민이 제조되는 방법.
  9. 제1항에 있어서, N-〔3-(1H-이미다졸-1-일)페닐〕-4-(2-퓨라닐)-2-피리미디나민이 제조되는 방법.
  10. 제1항에 있어서, N-〔3-(1H-이미다졸-1-일)페닐〕-4-(2-티에닐)-2-피리미디나민이 제조되는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019910006612A 1990-04-25 1991-04-24 N-[3-(1h-이미다졸-1-일)페닐]-4-(치환된)-2-피리미디나민 합성을 위한 개선된 방법 KR0168679B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US7/514,455 1990-04-25
US07/514,455 US5064963A (en) 1990-04-25 1990-04-25 Process for the synthesis of n-(3-(1h-imidazol-1-yl)phenyl-4-(substituted)-2-pyrimidinamines
US07/514,455 1990-04-25

Publications (2)

Publication Number Publication Date
KR910018375A true KR910018375A (ko) 1991-11-30
KR0168679B1 KR0168679B1 (ko) 1999-01-15

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KR1019910006612A KR0168679B1 (ko) 1990-04-25 1991-04-24 N-[3-(1h-이미다졸-1-일)페닐]-4-(치환된)-2-피리미디나민 합성을 위한 개선된 방법

Country Status (19)

Country Link
US (1) US5064963A (ko)
EP (1) EP0453731B1 (ko)
JP (1) JPH04225975A (ko)
KR (1) KR0168679B1 (ko)
AT (1) ATE170184T1 (ko)
AU (1) AU630849B2 (ko)
CA (1) CA2041031A1 (ko)
DE (1) DE69130029T2 (ko)
DK (1) DK0453731T3 (ko)
ES (1) ES2121757T3 (ko)
FI (1) FI100533B (ko)
GR (1) GR3027762T3 (ko)
HU (1) HU211774B (ko)
IE (1) IE911366A1 (ko)
NO (1) NO177567C (ko)
NZ (1) NZ237870A (ko)
SG (1) SG47565A1 (ko)
TW (1) TW215087B (ko)
ZA (1) ZA913092B (ko)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US5516775A (en) * 1992-08-31 1996-05-14 Ciba-Geigy Corporation Further use of pyrimidine derivatives
KR100643419B1 (ko) * 1998-03-27 2006-11-10 얀센 파마슈티카 엔.브이. Ｈｉｖ를 억제하는 피리미딘 유도체
BRPI0014271B1 (pt) 1999-09-24 2021-06-22 Janssen Pharmaceutica N.V. Partícula consistindo em uma dispersão de sólidos, uso da dita partícula, dispersão de sólidos, forma de dosagem farmacêutica, bem como processos de preparação de dita partícula, dispersão e forma de dosagem
EP1948647A1 (en) 2005-11-03 2008-07-30 SGX Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
JP2010526150A (ja) * 2007-05-04 2010-07-29 アイアールエム・リミテッド・ライアビリティ・カンパニー ｃ−ｋｉｔおよびＰＤＧＦＲキナーゼインヒビターとしての化合物および組成物
US9487504B2 (en) 2012-06-20 2016-11-08 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
WO2013192125A1 (en) * 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
CN110330447B (zh) * 2019-07-16 2022-04-15 北京赛升药业股份有限公司 一种甲磺酸萘莫司他中间体的制备方法及其应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU5319479A (en) * 1978-12-22 1980-06-26 Ici Australia Limited Pyrimidinyl amino phenoxy carboxylate derivatives
EP0164204A1 (en) * 1984-05-12 1985-12-11 FISONS plc Novel pharmaceutically useful pyrimidines
US4788195A (en) * 1986-01-13 1988-11-29 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines

Also Published As

Publication number Publication date
ZA913092B (en) 1992-02-26
HUT57719A (en) 1991-12-30
GR3027762T3 (en) 1998-11-30
ES2121757T3 (es) 1998-12-16
DK0453731T3 (da) 1999-02-15
NO911632D0 (no) 1991-04-24
DE69130029D1 (de) 1998-10-01
EP0453731A3 (en) 1992-09-02
NO177567C (no) 1995-10-11
CA2041031A1 (en) 1991-10-26
US5064963A (en) 1991-11-12
ATE170184T1 (de) 1998-09-15
KR0168679B1 (ko) 1999-01-15
IE911366A1 (en) 1991-11-06
NO177567B (no) 1995-07-03
TW215087B (ko) 1993-10-21
HU911373D0 (en) 1991-10-28
FI911983A0 (fi) 1991-04-24
NZ237870A (en) 1993-05-26
NO911632L (no) 1991-10-28
AU630849B2 (en) 1992-11-05
SG47565A1 (en) 1998-04-17
HU211774B (en) 1995-12-28
FI100533B (fi) 1997-12-31
AU7590591A (en) 1991-11-07
DE69130029T2 (de) 1999-02-18
FI911983A (fi) 1991-10-26
EP0453731B1 (en) 1998-08-26
JPH04225975A (ja) 1992-08-14
EP0453731A2 (en) 1991-10-30

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