KR940000461A - 4-하이드록시-5-할로피롤로［2,3-디］피리미딘 중간체의 합성 방법 - Google Patents

4-하이드록시-5-할로피롤로［2,3-디］피리미딘 중간체의 합성 방법 Download PDF

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KR940000461A
KR940000461A KR1019930011267A KR930011267A KR940000461A KR 940000461 A KR940000461 A KR 940000461A KR 1019930011267 A KR1019930011267 A KR 1019930011267A KR 930011267 A KR930011267 A KR 930011267A KR 940000461 A KR940000461 A KR 940000461A
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South Korea
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formula
defined above
pyrimidine
compound
reaction product
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KR1019930011267A
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KR100285891B1 (ko
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잭슨 바넷 찰스
에드워드 코비에르스키 마이클
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리로이 휘테커
일라이 릴리 앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

4-하이드록시피롤로〔2,3-d〕피리미딘을 불활성 유기용매의 존재하에 실리화하고, 요오드화, 브롬화 또는 염화시킴으로써 C-5 위치에 레지오선택적으로 할로겐화하였다.

Description

4-하이드록시-5-할로피롤로〔2,3-디〕피리미딘 중간체의 합성 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (2)

  1. (a)실리화제를 불화성 용기 용매의 존재하에하기 식의 4-하이드록시피롤로〔2,3-d〕피리미딘과 반응시키고
    [상기식에서, R은H, C1-C4알킬, C1-C4알콕시, 아릴, 벤질 또는 식 R1-NH-(여기에서, R1은 아미노보호그룹임)의 치환체이다〕; (b) 단계(a)의 반응 생성물을 요오드화, 브롬화 또는 염소화함을 포함하는, 하기 식의4-하이드록시 -5-할로피롤로〔2,3-d〕피리미딘의 제조방법.
    〔상기식에서, R은 상기에 정의된 바와 같고 X는 브로모, 클롤로 또는 요오드이다.
  2. (a) 실리화제를 불활성 유기 용매의 존재하에 하기 식의 4-하이드록시피롤로〔2,3-d〕피리미딘과 반응시키고
    (상기식에서, R은 H,C1-C4알킬, C1-C4알콕시, 아릴, 벤질 또는 식 R1-NH-(여기에서, R1은 아미노보호그룹임)의 치환체이다〕; (b) 단계(a)의 반응 생성물을 요오드화, 브롬화 또는 염소화하고; (c) 단계 (b)의 반응 생성물인 하기식의 화합물을
    〔상기식에서, R 및 R1은 상기에 정의된 바와 같고 X는 브로모, 클로로 또는 요오도이다〕
    하기식의 화합물과 축합시키고
    〔상기식에서, R2는 동일하거나 서로 다른 카복시 보호 그룹이고, *로표시된 탄소원자 주위의 배위는 이다〕
    (d) 단계 (c)의 반응 생성물인 하기식의 화합물을 수소화하고
    〔상기식에서, R, R1, R2및 *는 상기에 정의한 바와 같다〕; (e) 임의로 단계(d)의 반응 생성물을 약제학적으로 허용되는 염으로 전환시킴을 포함하는, 하기식의 화합물 또는 그의 염의 제조방법.
    〔상기식에서, R, R1, 및 *는 상기에 정의된 바와 같다〕
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019930011267A 1992-06-22 1993-06-19 4-하이드록시-5-할로피롤로(2,3-디)피리미딘 중간체의 합성 방법 KR100285891B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US902,116 1992-06-22
US07/902,116 US5235053A (en) 1992-06-22 1992-06-22 Process for the synthesis of 4-hydroxy-5-halopyrrold[2,3-d]pyrimidine intermediates

Publications (2)

Publication Number Publication Date
KR940000461A true KR940000461A (ko) 1994-01-03
KR100285891B1 KR100285891B1 (ko) 2001-04-16

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Family Applications (1)

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KR1019930011267A KR100285891B1 (ko) 1992-06-22 1993-06-19 4-하이드록시-5-할로피롤로(2,3-디)피리미딘 중간체의 합성 방법

Country Status (15)

Country Link
US (1) US5235053A (ko)
EP (1) EP0576211B1 (ko)
JP (1) JPH0656838A (ko)
KR (1) KR100285891B1 (ko)
AT (1) ATE204577T1 (ko)
BR (1) BR9302432A (ko)
CA (1) CA2098694A1 (ko)
DE (1) DE69330627T2 (ko)
DK (1) DK0576211T3 (ko)
ES (1) ES2160589T3 (ko)
HU (1) HU214019B (ko)
IL (3) IL119053A (ko)
MX (1) MX9303671A (ko)
PT (1) PT576211E (ko)
TW (1) TW226376B (ko)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL107041A (en) * 1992-09-25 2000-02-17 Lilly Co Eli Process for preparing omega(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo-6-¬2,3-d¾pyrimidin-5-YL)alkarylcarboxylic acids and N-(omega-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo¬2,3-d¾pyrimidin-5-YL)alk-aroyl-4-glutamic acids
US5426187A (en) * 1993-11-30 1995-06-20 Eli Lilly And Company Process for the preparation of 4-hydroxy-5-substituted ethynylpyrrolo [2,3-d]pyrimidine intermediates
US6002004A (en) * 1995-03-28 1999-12-14 Witco Vinyl Additives Gmbh Pyrrolodiazine derivatives as stabilizers for chilorine-containing polymers
JP3711238B2 (ja) * 1997-08-05 2005-11-02 ファイザー・プロダクツ・インク 神経ペプチドＹ受容体アンタゴニストとしての４−アミノピロ−ル（３，２−ｄ）ピリミジン
CN100374441C (zh) * 2003-06-06 2008-03-12 天津倍方科技发展有限公司 二氢吡咯[2，3-d]嘧啶-4-酮衍生物，其制备方法及其制药用途

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO169490C (no) 1988-03-24 1992-07-01 Takeda Chemical Industries Ltd Analogifremgangsmaate for fremstilling av terapeutisk aktive pyrrolopyrimidinderivater
IL96531A (en) * 1989-12-11 1995-08-31 Univ Princeton History of Acid N- (Diomeric-H1-Pyrolo] D-2,3 [Pyrimidine-3-Ilacyl (-glutamic, preparation and pharmaceutical preparations containing them)
US5028608A (en) 1989-12-11 1991-07-02 The Trustees Of Princeton University N-(6-Amino-(pyrrolo(2,3-d)pyrimidin-3-ylacyl) )-glutamic acid derivatives

Also Published As

Publication number Publication date
DK0576211T3 (da) 2001-10-08
US5235053A (en) 1993-08-10
JPH0656838A (ja) 1994-03-01
IL119053A (en) 1998-12-06
IL106054A0 (en) 1993-10-20
BR9302432A (pt) 1994-01-11
TW226376B (ko) 1994-07-11
IL119053A0 (en) 1996-11-14
EP0576211B1 (en) 2001-08-22
PT576211E (pt) 2001-12-28
MX9303671A (es) 1993-12-01
IL106054A (en) 1997-07-13
EP0576211A3 (en) 1994-06-15
ES2160589T3 (es) 2001-11-16
CA2098694A1 (en) 1993-12-23
HUT65439A (en) 1994-06-28
DE69330627T2 (de) 2002-06-13
KR100285891B1 (ko) 2001-04-16
EP0576211A2 (en) 1993-12-29
DE69330627D1 (de) 2001-09-27
HU214019B (hu) 2000-06-28
HU9301829D0 (en) 1993-09-28
ATE204577T1 (de) 2001-09-15

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