KR830003475A - 신규의 피리미돈류의 제조방법 - Google Patents

신규의 피리미돈류의 제조방법 Download PDF

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KR830003475A
KR830003475A KR1019800003257A KR800003257A KR830003475A KR 830003475 A KR830003475 A KR 830003475A KR 1019800003257 A KR1019800003257 A KR 1019800003257A KR 800003257 A KR800003257 A KR 800003257A KR 830003475 A KR830003475 A KR 830003475A
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alkoxy
formula
methyl
alkyl
group
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KR1019800003257A
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KR840002174B1 (ko
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헨리 브라운 토마스
조세프 킹 로날드
레이몬드 화이트 죠지
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죤 안토니 클래이스
스미스클라인 앤드 프렌취 레버러토리이스 리미티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
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    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

내용 없음

Description

신규의 피리미돈류의 제조방법.
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 하기구조식(1)의 화합물의 제조공정.
    및 그것의 산부가염류, 윗식에서 Het는 치환물(동일하거나 서로 다를 수 있음)이하나 또는 그 이상의 C1-4알킬, 삼플루오로메틸, 할로겐, 히드록시, C1-4알콕시 또는 아미노기인 헤테로시클릭기를 함유한 임의치환된 5- 또는 6의 원소의 완전히 불포환된 질소임 ; n은 2또는 3임 ; Z는 수소 또는 C1-4알킬 ; A는 산소 또는 황으로 임의 저해된 C1-5알킬렌이며 B는 수소, 메틸, C3-6시클로알킬, 치환물(동일하거나 서로 다를수 있음)이 하나 또는 그 이상의 C1-4알킬, C1-4알콕시, 또는 수산기인 임의치환된 헤테로알릴기임 ; 또는 B는 나프틸, 5-또는 6-(2,3-디히드로-1,4-벤조디옥시닐)또는 4-또는 5-(1,3-벤조디옥실릴)기 또는 치환물 (동일하거나 서로 다를 수 있음)이 하나 또는 그 이상의 C1-4알킬, C1-4알콕시, 할로겐, 알릴-(C1-4알콕시), 수산, C1-4알콕시-C1-4알콕시, 삼플루오로메틸, 디(C1-4알킬)아미노, 페녹시, 할로페녹시, 또는 하기구조식(4)로 특징지어진 C1-4알콕시 페닐기인 임의치환된 페닐기임 : -
    Het-CH2L(4) (4)
    또는 Het는 반응을 저해하는 어떠한 치환물도 저해되었다는 가정하에 구조식(1)에서 정의한 대로이며 L은 티올과 대치할 수 있는 기인 하기구조식(5)의 화합물과 반응한 그것의 산부가염 : -
    또는 n, Z, A 및 B는 B내의 어떠한 페놀수산기도 임의로 저해되었고, 그후 저해기를 제거하고 이생산물을 부가염으로 전화시켰다는 가정하에서 구조식(1)에 정의한 대로인 그것의 산부가염.
  2. L이 수산, 아세톡시, 메탄설포닐옥시, P-톨루엔설포닐 옥시, 메톡시, 염소, 브롬, 또는 트리페닐포스포늄인데에 특징이 있는 청구범위 10에 청구한대로의 공정.
  3. L이 수산 또는 C1-4알콕시 및 반응이 산성조건하에 수행되는데에 특징이 있는 청구범위 1또는 청구범위 2에 청구된 대로의 공정.
  4. Het 또는 B가 산변화성, L이 염소 또는 브롬이고, 반응이 염기의 존재하에 수행되는데에 특징이 있는 청구범위 1또는 청구범위 2에 청구된대로의 공정.
  5. 생산물이 2-[2-(5-메틸-4-이미다졸릴메틸티오)에틸아미노]-5-(3-메톡시벤질)-4-피리미돈, 2-[2-(5-메틸-4-이미다졸릴메틸티오)에틸아미노]-5-[5-(1,3-벤조디옥솔릴메틸)-4-피리미돈 및 2-[2-(5-메틸-4-이미다졸릴 메틸티오)에틸아미노]-5-(3-피리딜메틸)-4-피리미돈 및 2-[2-(5-메틸-4-이미다졸릴 메틸티오)에틸아미노]-5-(6-메틸-3-피리딜메틸)-4-피리미돈인 데에 특징이있는 청구범위 1 또는 청구범위 2에 청구된대로의 공정.
  6. 반응이 산성미디엄에서 수행되며 구조식(5)의 화합물이 하기의 구조식(5나)의 화합물로부터 그 자체내에서 생성되는데에 특징이있는 청구범위 1에서 3 및 5중 어느것에 청구된 대로의 공정 :
    윗식에서 n, Z, A 및 B는 구조식(1)에서 정의한 대로이며 G'는 산변화성-저해기임.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019800003257A 1979-08-21 1980-08-19 신규의 피리미돈류의 제조방법 KR840002174B1 (ko)

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GB7929012 1979-08-21
GB7929012 1979-08-21

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KR830003475A true KR830003475A (ko) 1983-06-20
KR840002174B1 KR840002174B1 (ko) 1984-11-26

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EP (1) EP0024873A1 (ko)
JP (1) JPS5630975A (ko)
KR (1) KR840002174B1 (ko)
CA (1) CA1140129A (ko)
HU (1) HU184816B (ko)
IL (1) IL60862A0 (ko)
YU (1) YU210180A (ko)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4439609A (en) * 1980-10-01 1984-03-27 Smith Kline & French Laboratories Limited Pyridines
ZW21281A1 (en) * 1980-10-01 1981-11-18 Smith Kline French Lab Amine derivatives
US4352933A (en) * 1981-02-06 1982-10-05 Smithkline Beckman Corporation Chemical methods and intermediates for preparing substituted pyrimidinones
ATE21901T1 (de) * 1982-07-30 1986-09-15 Smith Kline French Lab Aminopyrimidinone und ihre herstellung.
US4772704A (en) * 1983-09-21 1988-09-20 Bristol-Myers Company 2,5-disubstituted-4(3H)-pyrimidones having histamine H2 -receptor antagonist activity
JP2003019317A (ja) * 2001-07-06 2003-01-21 Toyomaru Industry Co Ltd 遊技機

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL57005A (en) * 1978-04-11 1983-11-30 Smith Kline French Lab Process for the preparation of 2-amino pyrimid-4-one derivatives and novel 2-nitroaminopyrimid-4-ones as intermediates therefor
US4496567A (en) * 1978-11-13 1985-01-29 Smith Kline & French Laboratories Limited Phenyl alkylaminopyrimidones

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EP0024873A1 (en) 1981-03-11
YU210180A (en) 1983-06-30
HU184816B (en) 1984-10-29
IL60862A0 (en) 1980-10-26
CA1140129A (en) 1983-01-25
JPS5630975A (en) 1981-03-28
KR840002174B1 (ko) 1984-11-26

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