KR970074772A - Novel pyrimidine derivatives and processes for their preparation - Google Patents

Novel pyrimidine derivatives and processes for their preparation Download PDF

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Publication number
KR970074772A
KR970074772A KR1019960014539A KR19960014539A KR970074772A KR 970074772 A KR970074772 A KR 970074772A KR 1019960014539 A KR1019960014539 A KR 1019960014539A KR 19960014539 A KR19960014539 A KR 19960014539A KR 970074772 A KR970074772 A KR 970074772A
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KR
South Korea
Prior art keywords
dimethylpyrimidine
fluorophenylamino
hydroxy
preparation
processes
Prior art date
Application number
KR1019960014539A
Other languages
Korean (ko)
Other versions
KR0177293B1 (en
Inventor
홍유화
이영남
김홍배
Original Assignee
김태훈
주식회사 유한양행
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to KR1019960014539A priority Critical patent/KR0177293B1/en
Application filed by 김태훈, 주식회사 유한양행 filed Critical 김태훈
Priority to PCT/KR1997/000073 priority patent/WO1997042186A1/en
Priority to CNB021247854A priority patent/CN1190427C/en
Priority to AT97920966T priority patent/ATE206117T1/en
Priority to EP97920966A priority patent/EP0900214B1/en
Priority to PT97920966T priority patent/PT900214E/en
Priority to DE69706981T priority patent/DE69706981T2/en
Priority to AU27133/97A priority patent/AU712970B2/en
Priority to US09/171,579 priority patent/US5990311A/en
Priority to JP53975697A priority patent/JP3160297B2/en
Priority to CA002358479A priority patent/CA2358479C/en
Priority to CA002253906A priority patent/CA2253906C/en
Priority to RU98121687/04A priority patent/RU2174978C2/en
Priority to DK97920966T priority patent/DK0900214T3/en
Priority to ES97920966T priority patent/ES2165052T3/en
Priority to CN97194367A priority patent/CN1097591C/en
Publication of KR970074772A publication Critical patent/KR970074772A/en
Application granted granted Critical
Publication of KR0177293B1 publication Critical patent/KR0177293B1/en
Priority to HK99104379A priority patent/HK1019336A1/en
Priority to JP2000198538A priority patent/JP2001055379A/en
Priority to US09/667,428 priority patent/US6252076B1/en

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • 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
    • C07D239/30—Halogen atoms or nitro radicals
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

본 발명은 우수한 가역적인 프로톤펌프 저해효과로 위산분비를 효과적으로 억제하여 항궤양제로 사용가능한 5, 6-디메틸-2-(4-플루오로페닐아미노)-4-(1-메틸-1,2,3,4-테트라히드로이소퀴놀린-2-일) 피리미딘·염산염의 제조중간체로서 유용한 하기 일반식(Ⅰ)의 신규의 피리미딘 유도체 및 그의 제조방법에 관한 것이다.The present invention relates to a method for inhibiting gastric acid secretion by effectively inhibiting the secretion of 5-ethyl-2- (4-fluorophenylamino) -4- (1-methyl- 3,4-tetrahydroisoquinolin-2-yl) pyrimidine hydrochloride, which is useful as an intermediate for the preparation of the novel pyrimidine derivative of the following formula (I) and a process for producing the same.

( (

여기서, R은 히드록시 또는 할로겐이다.Wherein R is hydroxy or halogen.

Description

신규의 피리미딘 유도체 및 그의 제조방법Novel pyrimidine derivatives and processes for their preparation

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is a trivial issue, I did not include the contents of the text.

Claims (4)

하기 일반식(Ⅰ)의 피리미딘 유도체.A pyrimidine derivative of the general formula (I) 여기서 R은 히드록시 또는 할로겐이다.Wherein R is hydroxy or halogen. 4-플루오로페닐구아니딘·카보네이트를 에틸 2-메틸아세토아세테이트와 반응시키는 것을 특징으로 하는 4-히드록시-2-(4-플루오로페닐아미노)-5, 6-디메틸피리미딘의 제조방법.A process for producing 4-hydroxy-2- (4-fluorophenylamino) -5,6-dimethylpyrimidine, characterized in that 4-fluorophenylguanidine carbonate is reacted with ethyl 2-methylacetoacetate. 4-플루오로페닐구아니딘·카보네이트를 에틸 2-메틸아세트아세테이트와 반응시키고, 4-히드록시-2-(4-츨루오로페닐아미노)-5, 6-디메틸피리미딘을 분리하거나 분리함이 없이, 할로겐화제를 반응시키는 것을 특징으로 하는 하기 일반식(Ⅱ)의 4-할로게노-2-(4-플루오로페닐아미노)-5, 6-디메틸피리미딘의 제조방법.4-fluorophenylguanidine carbonate was reacted with ethyl 2-methylacetate to give 4-hydroxy-2- (4-chlorophenylamino) -5,6-dimethylpyrimidine (4-fluorophenylamino) -5,6-dimethylpyrimidine represented by the following general formula (II), wherein the halogenating agent is reacted with a halogenating agent. 여기서 Hal은 할로겐을 나타낸다.Wherein Hal represents halogen. 4-히드록시-2-(4-플루오로페닐아미노)-5, 6-디메틸피리미딘과 할로겐화제를 반응시키는 것을 특징으로 하는 하기 일반식(Ⅱ)의 4-할로게노-2-(4-플루오로페닐아미노)-5, 6-디메틸피리미딘의 제조방법.4-halogeno-2- (4-fluorophenylamino) -5,6-dimethylpyrimidine of the following formula (II), which is characterized in that 4-hydroxy-2- Fluorophenylamino) -5,6-dimethylpyrimidine. 여기서 Hal은 할로겐을 나타낸다.Wherein Hal represents halogen. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: It is disclosed by the contents of the first application.
KR1019960014539A 1996-05-04 1996-05-04 Novel pyrimidine derivatives and the process for preparing thereof KR0177293B1 (en)

Priority Applications (19)

Application Number Priority Date Filing Date Title
KR1019960014539A KR0177293B1 (en) 1996-05-04 1996-05-04 Novel pyrimidine derivatives and the process for preparing thereof
RU98121687/04A RU2174978C2 (en) 1996-05-04 1997-04-30 Method of synthesis of pyrimidine derivative, intermediate compounds and method of their synthesis
AT97920966T ATE206117T1 (en) 1996-05-04 1997-04-30 METHOD FOR PRODUCING PYRIMIDINE DERIVATIVES
EP97920966A EP0900214B1 (en) 1996-05-04 1997-04-30 Process for preparation of pyrimidine derivatives
PT97920966T PT900214E (en) 1996-05-04 1997-04-30 PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES
DE69706981T DE69706981T2 (en) 1996-05-04 1997-04-30 METHOD FOR PRODUCING PYRIMIDINE DERIVATIVES
AU27133/97A AU712970B2 (en) 1996-05-04 1997-04-30 Process for preparation of pyrimidine derivatives
US09/171,579 US5990311A (en) 1996-05-04 1997-04-30 Process for preparation of pyrimidine derivatives
PCT/KR1997/000073 WO1997042186A1 (en) 1996-05-04 1997-04-30 Process for preparation of pyrimidine derivatives
CA002358479A CA2358479C (en) 1996-05-04 1997-04-30 4-substituted-2-(4-fluorophenylamino)-5,6 dimethylpyrimidine
CA002253906A CA2253906C (en) 1996-05-04 1997-04-30 Process for preparation of pyrimidine derivatives
CNB021247854A CN1190427C (en) 1996-05-04 1997-04-30 Method for preparing pyrimidine derivative
DK97920966T DK0900214T3 (en) 1996-05-04 1997-04-30 Process for Preparation of Pyrmidine Derivatives
ES97920966T ES2165052T3 (en) 1996-05-04 1997-04-30 PROCEDURE FOR THE PREPARATION OF PIRIMIDINE DERIVATIVES.
CN97194367A CN1097591C (en) 1996-05-04 1997-04-30 Process for preparing pyrimidine derivatives
JP53975697A JP3160297B2 (en) 1996-05-04 1997-04-30 Method for producing pyrimidine derivative
HK99104379A HK1019336A1 (en) 1996-05-04 1999-10-07 Process for preparation of pyrimidine derivatives
JP2000198538A JP2001055379A (en) 1996-05-04 2000-06-30 Production of 1-methyl-1,2,3,4-tetrahydroisoquinoline
US09/667,428 US6252076B1 (en) 1996-05-04 2000-09-21 Process for preparation of pyrimidine derivatives

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019960014539A KR0177293B1 (en) 1996-05-04 1996-05-04 Novel pyrimidine derivatives and the process for preparing thereof

Publications (2)

Publication Number Publication Date
KR970074772A true KR970074772A (en) 1997-12-10
KR0177293B1 KR0177293B1 (en) 1999-03-20

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KR1019960014539A KR0177293B1 (en) 1996-05-04 1996-05-04 Novel pyrimidine derivatives and the process for preparing thereof

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