KR830007602A - N-티아졸릴메틸 티오알킬-n'-알킬아미딘의 제조방법 - Google Patents

N-티아졸릴메틸 티오알킬-n'-알킬아미딘의 제조방법 Download PDF

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KR830007602A
KR830007602A KR1019810003721A KR810003721A KR830007602A KR 830007602 A KR830007602 A KR 830007602A KR 1019810003721 A KR1019810003721 A KR 1019810003721A KR 810003721 A KR810003721 A KR 810003721A KR 830007602 A KR830007602 A KR 830007602A
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alkyl
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hydrogen
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KR850001795B1 (ko
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폴 피오취 리챠드
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아더 알·웨일
일라이 릴리앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

N-티아졸릴메틸 티오알킬-N1-제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. (a) 다음 일반식(Ⅱ)의 아민을(i) 일반식 L1QB(L1은 이탈기)의 화합물 또는 (ii) 일반식 R6-N=C=A의 화합물과 반응시켜 Q가 -C=A이고 R 이 수소인 일반식(I)의 화합물을 제조하거나,
    (b) 다음 일반식(Ⅲ)의 화합물을 일반식 HNRR6의 아민과 반응시키거나,
    (c) 다음 일반식(Ⅳ)의 화합물을 일반식 R2NH2의 아민과 반응시켜 Q가 C=A인 일반식(I)의 티아졸을 제조하거나,
    (d)다음 일반식(Ⅴ)의 화합물을 일반식(Ⅵ)의 티올과 융합시켜 Z은 황이고, Q는 C=A인 일반식(I) 의 화합물을 제조함을 특징으로 하여 다음 일반식(I)의 화합물 및 이들의 약학적으로 무독한 염을 제조하는 방법.
    상기 일반식에서
    R1과 R2는 각각 수소, C1-4알킬, 벤질 또는 벤조일을 나타내거나 또는 인접해 있는 질소와 함께 탄소수 5 내지 7의 포화 복소환 기를 나타내며,
    R3는 수소 또는 C1-4알킬,
    z는 O, S 또는 CH2;
    n은 Z가 0 또는 S일 때는 2 또는 3이고, Z가 CH2일 때는 1,2 또는 3이며,
    R5는 수소 또는 C1-4알킬;
    m은 1, 2 또는 3;
    Q는또는이며, 여기서 A는 N-CN, N-NO2,CH-NO2, S, O, NHH, N-SO2-아릴, N-SO2-C1-4알킬, N-CO-NH2, N-CO-C1-4-알킬, N-CO2-C1-4-알킬, CH-SO2-아릴 또는 CH-SO2-C1-4-알킬, (아릴올 페닐, 할로페닐, C1-4알킬페닐 또는 C1-4알콕시페닐)이고,
    B는 NRR6이고;
    여기서 R과 R6는 각각 수소 또는 C1-5알킬, C3-6사이클로알킬메틸, 하이드록시 C2-5알킬, C3-6사이클로 알킬, 알콕시알킬 또는 디알킬아미노알킬이며, 탄소의 총수는 8보다 적으며, 복소원자 사이에서 적어도 2개의 탄소가 있어야하며,
    L2는 이탈그룹,
    L3는 이탈그룹을 나타낸다.
  2. 제1항에 있어서, R1과 R2는 각각 수소 또는 C1-3알칼을 나타내고 R1과 R2중 하나만이 벤질 또는 벤조일을 나타낼 수 있으며, 또는 R1과 R2가 인접한 질소와 함께 피레리디노, 피롤리디노 또는 모르폴리노 그룹을 나타내며, 단 Z가 CH2일 때는 R1과 R2중 하나만이 수소를 나타낼 수 있으며, R3는 수소 또는 C1-3알킬, R4는 C1-5알킬, R5는 수소 또는 메틸;
    A는 N-CN, N-NO2,CH-NO2, S, O, NH, N-SO2-아릴, N-SO2-C1-3알킬, N-CO-NH2, N-(O-C1-3알킬, N-CO2-C1-3-알킬, CH-SO2-아릴 또는 CH-SO2-CH3이고, 여기서 아릴은 페닐, 할로페닐, C1-3알킬페닐, 또는 C1-3알콕시페닐, R6는 수소, Q는 C=A인 일반식(I)의 티아졸 유도체 또는 이들의 약학적으로 무독한 산부가염.
  3. 제1항에 있어서 N-메틸-N′-2-([2-(디메틸아미노메틸)-4-티아졸린]메틸티오)에틸-N″-시아노구아니딘 또는 이들의 약학적으로 무독한 염을 제조하는 방법.
  4. 제1항에 있어서 N-메틸-N′-2-([2-(디메틸아미노메틸)-4-티아졸릴]메틸티오)에틸-2-니트로-1,1-에텐디아민 또는 이들의 약학적으로 무독한 염을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810003721A 1980-10-02 1981-10-02 2,4-이치환된 티아졸 유도체의 제조방법 KR850001795B1 (ko)

Applications Claiming Priority (2)

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US06/193,192 US4375547A (en) 1980-10-02 1980-10-02 N-Methyl-N'-2-([(2-dimethylaminomethyl)-4-thiazolyl]methylthio)ethyl 2-nitro-1,1-ethenediamine
US193,192 1980-10-02

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KR850001795B1 KR850001795B1 (ko) 1985-12-21

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JP (1) JPS5791980A (ko)
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AR (1) AR241439A1 (ko)
AU (1) AU542553B2 (ko)
BG (1) BG60249B1 (ko)
CA (1) CA1166248A (ko)
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DD (1) DD200371A5 (ko)
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FI76570C (fi) 1988-11-10
RO85815A (ro) 1984-11-25
SU1184443A3 (ru) 1985-10-07
IE812285L (en) 1982-04-02
NO813334L (no) 1982-04-05
GB2084581B (en) 1985-02-27
GR75023B (ko) 1984-07-12
IE51603B1 (en) 1987-01-21
PT73757A (en) 1981-11-01
GB2084581A (en) 1982-04-15
PL238035A1 (en) 1983-02-28
RO85815B (ro) 1984-11-30
DK12391D0 (da) 1991-01-24
AU542553B2 (en) 1985-02-28
YU42728B (en) 1988-12-31
IL63980A0 (en) 1982-01-31
ZA816817B (en) 1983-05-25
JPS5791980A (en) 1982-06-08
BG60249B2 (en) 1994-03-24
KR850001795B1 (ko) 1985-12-21
RO82215B (ro) 1983-06-30
US4375547A (en) 1983-03-01
HK15987A (en) 1987-02-27
DK435181A (da) 1982-05-12
DK164056B (da) 1992-05-04
EP0049618A1 (en) 1982-04-14
MY8700247A (en) 1987-12-31
NO155885C (no) 1987-06-17
BG60249B1 (bg) 1994-03-24
PH18135A (en) 1985-04-03
YU236481A (en) 1983-10-31
ES8306135A1 (es) 1983-05-01
CA1166248A (en) 1984-04-24
IL63980A (en) 1986-04-29
LU88293I2 (fr) 1994-05-04
UA6081A1 (uk) 1994-12-29
RO82215A (ro) 1983-07-07
PL130526B1 (en) 1984-08-31
PL233295A1 (ko) 1982-12-20
EP0049618B1 (en) 1985-08-14
PT73757B (en) 1983-01-13
FI813058L (fi) 1982-04-03
NL930107I2 (nl) 1997-02-03
DK167759B1 (da) 1993-12-13
MX5723A (es) 1993-12-01
CS227015B2 (en) 1984-04-16
CY1351A (en) 1987-04-24
ES505950A0 (es) 1983-01-01
NO155885B (no) 1987-03-09
ES8301950A1 (es) 1983-01-01
ES514868A0 (es) 1983-05-01
DD200371A5 (de) 1983-04-20
DK12391A (da) 1991-01-24
NL930107I1 (nl) 1993-10-18
JPH021141B2 (ko) 1990-01-10
AU7594581A (en) 1982-04-08
HU188697B (en) 1986-05-28
NZ198523A (en) 1985-12-13
AR241439A1 (es) 1992-07-31
EG15678A (en) 1986-12-30
DK164056C (da) 1992-09-28
PL130626B1 (en) 1984-08-31
DE3171819D1 (en) 1985-09-19

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