KR860000285A - 1,4-디하이드로피리딘 유도체의 제조방법 - Google Patents

1,4-디하이드로피리딘 유도체의 제조방법 Download PDF

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Publication number
KR860000285A
KR860000285A KR1019850004165A KR850004165A KR860000285A KR 860000285 A KR860000285 A KR 860000285A KR 1019850004165 A KR1019850004165 A KR 1019850004165A KR 850004165 A KR850004165 A KR 850004165A KR 860000285 A KR860000285 A KR 860000285A
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alkyl
substituted
compound
ring
hydroxy
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KR1019850004165A
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앨커 디. (외 2)
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윌리암 죤 윌슨
화이자 코포레이션
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Publication of KR860000285A publication Critical patent/KR860000285A/ko

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    • 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
    • C07D401/12—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 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
    • C07D401/02—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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • General Health & Medical Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

내용 없음

Description

1,4-디하이드로피리딘 유도체의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (13)

  1. 일반식(Ⅱ)의 화합물을 X1이 할로겐 또는 S-(C1내지C4)알킬로 치환된경 우에는 일반식 R3O-의 알콕사이드와 반응시키거나, X1이 OH로 치환된 경우에는 트리알킬옥소늄 테트라플루오로보레이트와 반응시키거나; 일반식(Ⅳ)의 화합물을 O-메틸이소우레아 하이드로겐설페이트와 반응시켜 X가 2-메톡시-4피리미돈-6-일인 화합물을 생성시키고; 임의로 수득된 생성물을 약제학적으로 무독한 염으로 전환시킴을 특징으로 하여, 일반식(Ⅰ)의 화합물 및 그의 약제학적으로 무독한 염을 제조하는 방법.
  2. (Ⅰ)
  3. (Ⅱ)
  4. (Ⅳ)
  5. 상기식에서 R은 아릴 또는 헤테로아릴이고, R1및 R2는 각기 독립적으로 (C1내지C4)알킬 또는 2-메톡시에틸이며; X는 한개이상의 OR3그룹으로 치환되고, 임의로 하나이상의((C1내지C4)알킬, 아릴, 하이드록시, 옥소, CN,N(R4)2,(CH2)mCON(R4)2또는 (CH2)mCO2R5그룹에 의해 추가로 치환될 수 있는 5또는 6-원, 질소-함유 방향족 헤테로사이클릭환이고, 여기서 R3는(C1내지C4)알킬이며, R4는 각기 독립적으로 H또는 (C1내지C4)알킬이거나, 2개의 그룹 R4가 이들이 결합된 질소원자와 함께는 피롤리디닐, 피페리디노, 모르폴리노, 피페라지닐 또는 N-(C1내지 C4)알킬-피페라지닐 그룹을 형성하고, R5는 H 또는 ((C1내지 C4)알킬이며, m은 0또는 1이고; Y는 -(CH2)n-,-CH2CH(CH3)- 또는 CH2C(CH3)2-이며, 여기에서 n은 X가 환탄소원자를 통해 Y에 결합된 경우에는 1내지 3이고, X가 환질소원자를 통해 Y에 결합된 경와에는 2또는 3이며;X1은 환에 OR3치환체 그룹을 함유하지 않고, 대신에 환이 할로겐(특히 염소),S(C1내지C4)알킬 또는 하이드록시로 치환되는 것을 제외하고는, X에 대해 정의한 바와 같은 5-또는 6-원 질소- 함유 헤테로사이클릭 그룹이고; R6는(C1내지C4)알킬이다.
  6. 제1항에 있어서, R이 2-클로로페닐 또는 2,3- 디클로로페닐인 방법.
  7. 제1또는 2항에 있어서, R1및 R2가 CH2이고, X의 환탄소원자에 결합하는 방법.
  8. 제1 내지 3항중 어느 한항에 있어서, Y가 CH2이고, X의 환탄소원자에 결합하는 방법.
  9. 제1내지 4항중 어느 한항에 있어서, X가 하나 또는 2개의 (C1내지C4)알콕시그룹에 의해 치환되며, 임의로 아미노,(C1내지C4)알킬, 하이드록시 또는 옥소그룹에 의해 추가로 치환된 피리미디닐, 피라졸리닐, 아미다졸릴 또는 트리아졸릴인 방법.
  10. 제5항에 있어서, X가 4-메톡시-2-메틸피미리딘-6-일,4-이소프로폭시-2메틸피리미딘-6-일, 2-아미노-4-메톡시피리미딘-6-일,2-메톡시-4-프리미돈-6-일 또는 2,4-디메톡시피리미딘-6-일인 방법.
  11. 제1항에 있어서, X1은 염소로 치환되고, 반응을 메탄올중, 실온에서 나트륨 메톡사이드를 사용하여 수행하는 방법.
  12. 제1항에 있어서, X1이 하이드록시로 치환되고, 반응을 디클로로메탄중, 0℃ 내지 실온에서 트리메틸옥소늄 테트라플루오로보레이즈를 사용하여 수행하는 방법.
  13. ※ 참고사항 : 최초출원내용에 의하여 공개하는 것임.
KR1019850004165A 1984-06-15 1985-06-13 1,4-디하이드로피리딘 유도체의 제조방법 KR860000285A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB8415386 1984-06-15
GB848415386A GB8415386D0 (en) 1984-06-15 1984-06-15 Therapeutic agents

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KR860000285A true KR860000285A (ko) 1986-01-27

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KR1019850004165A KR860000285A (ko) 1984-06-15 1985-06-13 1,4-디하이드로피리딘 유도체의 제조방법

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Country Link
EP (1) EP0165032A3 (ko)
JP (1) JPS617276A (ko)
KR (1) KR860000285A (ko)
AU (1) AU4368985A (ko)
DK (1) DK269885A (ko)
FI (1) FI852340L (ko)
GB (1) GB8415386D0 (ko)
GR (1) GR851447B (ko)
HU (1) HUT37934A (ko)
IL (1) IL75507A0 (ko)
PT (1) PT80630B (ko)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1213555B (it) * 1986-12-11 1989-12-20 Boehringer Biochemia Srl 2 metiltiometildiidropiridine, un processo per laloro preparazione e composizioni farmaceutiche che le contengono.

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE7910521L (sv) * 1979-12-20 1981-06-21 Haessle Ab Nya 2-metyl-6-substituerade-4-(2,3-disubstituerad fenyl)-1,4-dihydropyridin-3,5-diestrar med hypotesiva egenskaper, samt forfarande for deras framstellning, och farmaceutiska beredningar innehallande desamma
CS228917B2 (en) * 1981-03-14 1984-05-14 Pfizer Method of preparing substituted derivatives of 1,4-dihydropyridine
NZ201395A (en) * 1981-07-30 1987-02-20 Bayer Ag Pharmaceutical compositions containing 1,4-dihydropyridines and certain of these dihydropyridines
DE3207982A1 (de) * 1982-03-05 1983-09-08 Bayer Ag, 5090 Leverkusen Neue 1,4-dihydropyridine, verfahren zu ihrer herstellung und ihrer verwendung in arzneimitteln
DE3363743D1 (en) * 1982-07-22 1986-07-03 Pfizer Ltd Dihydropyridine anti-ischaemic and antihypertensive agents
EP0107293A3 (en) * 1982-09-04 1984-06-06 Pfizer Limited Dihydropyridines
PH19166A (en) * 1982-09-04 1986-01-16 Pfizer Dihydropyridined,pharmaceutical compositions and method of use
US4515799A (en) * 1983-02-02 1985-05-07 Pfizer Inc. Dihydropyridine anti-ischaemic and antihypertensive agents

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Publication number Publication date
FI852340A0 (fi) 1985-06-12
JPS617276A (ja) 1986-01-13
DK269885D0 (da) 1985-06-14
EP0165032A2 (en) 1985-12-18
AU4368985A (en) 1985-12-19
PT80630B (en) 1987-04-28
HUT37934A (en) 1986-03-28
DK269885A (da) 1985-12-16
GR851447B (ko) 1985-11-25
GB8415386D0 (en) 1984-07-18
EP0165032A3 (en) 1987-06-16
FI852340L (fi) 1985-12-16
IL75507A0 (en) 1985-10-31
PT80630A (en) 1985-07-01

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