KR830004300A - 벤조디아제핀 화합물의 제조방법 - Google Patents

벤조디아제핀 화합물의 제조방법 Download PDF

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Publication number
KR830004300A
KR830004300A KR1019800003960A KR800003960A KR830004300A KR 830004300 A KR830004300 A KR 830004300A KR 1019800003960 A KR1019800003960 A KR 1019800003960A KR 800003960 A KR800003960 A KR 800003960A KR 830004300 A KR830004300 A KR 830004300A
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South Korea
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alkyl
hydrogen
cycloalkyl
general formula
halogen
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KR1019800003960A
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KR850000471B1 (ko
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쿠마 차크라바아리 지반
미첼 호텐 테렌스
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케네스 윌리암 헨리 맥베이
릴리 인더스트리스 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C07D231/38—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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

내용 없음

Description

벤조디아제핀 화합물의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (7)

  1. (가) 일반식 R5H의 아민을 다음 일반식으로 표시되는 화합물과 반응시키거나
    여기서 Q는 아민 R5H의 수소원자를 분리할 수 있는 기를 나타내고, R6또는 R9이 수소이면 일반식 R6X 또는 R9X의 화합물과 반응시키고, X는 이탈기이고, n가 0이면 산화시킨다.
    (나) 다음 일반식의 화합물을 폐환시켜서 제조함을
    (R6와 R9가 수소이면, 일반식 R6X와 R9X와 반응시키고 X는 이탈기이고, n가 0이면 산화시킨다)
    특징으로 하는 하기 일반식(Ⅰ)으로 표시되는 화합물 또는 이의 산부가염의 제조방법.
    (상기 식에서 R1,R2,R3와 R10는 각각 수소, C1-4알킬, C2-4알켄일, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬, 할로겐, C1-4할로알킬, C1-4알카노일, 니트로, 아미노, C2-4아실아미노, 시아노, 히드록실, C1-4알콕시, C1-4알킬티오, C1-4할로알콕시 또는 일반식 -SO2N(R8)2, -S02R8또는 -S03R8를 나타내고 여기서 R8은 C1-4알킬, C1-4할로알킬 또는 임의로 치환된 페닐이고; QR5는 다음 일반식의 기이다.
    여기서 R9는 할로겐, C1-4알킬, C3-7싸이클로알킬, C3-7싸이클로알킬, C1-4알킬, C1-4할로알킬, C2-4알켄일, C1-4알카노일, 벤질, 시아노- 또는 임의로 치환된 페닐이고 R10은 수소, C1-4알킬 또는 임의로 치환된 페닐이고, n는 0 또는 1이다; R6는 수소, C1-10알킬, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬, C1-4할로알킬, 벤질, C1-6알카노일, C1-4카르브알콕시 또는 벤조일이고, R7은 R6중의 하나 또는 할로겐, 니트로, 시아노, 아미노 또는 C1-4아실아미노이다).
  2. R1,R2와 R3가 각각 수소, C1-4알킬, C2-4알켄일, 할로겐, C1-4할로알킬, 니트로, C1-4알콕시, C1-4할로알콕시, C1-4알킬티오, C1-4할로알킬설폰일 또는 페닐설폰일이고, R4는 수소이고, R6가 수소, C1-10알킬, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬 또는 벤질이고, R7가 수소 또는 C1-10알킬이고, R9이 수소, C1-4알킬, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬 또는 벤질이고, R10이 수소 또는 C1-4알킬인 화합물을 제조하기 위한 청구범위 1에 따른 방법.
  3. 다음 일반식의 화합물을 제조하기 위한 청구범위 1에 따른 방법.
    (상기식에서 R1,R2와 R3가 각각 수소, C1-4알킬, C2-4알켄일, 할로겐, C1-4할로알킬, 니트로, C1-4알콕시, C1-4알킬티오 또는 페닐설폰일이고, R6는 수소, C1-10알킬, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬 또는 벤질이고, R7은 수소 또는 C1-10알킬이고, R9은 수소, C1-4알킬, C3-7싸이클로알킬, C3-7싸이클로알킬 C1-4알킬 또는 벤질을 나타낸다).
  4. R1,R2와 R3가 각각 수소, 할로겐 또는 C1-4할로알킬을 나타내고, R6가 C1-6알킬, C3-7싸이클로알킬 또는 C3-7싸이클로알킬 C1-4알킬이고, R7은 수소이고 R9는 수소, C1-4알킬, C3-7싸이클로알킬 C1-4알킬 또는 벤질인 화합물을 제조하기 위한 청구범위 3에 따른 방법.
  5. R2가 할로겐이고 R1과 R3가 수소이고 또한 R2와 R3가 할로겐이고, R1이 수소이고, R6가 메틸 또는 에틸이고 R7이 수소이고, R9이 메틸인 화합물을 제조하기 위한 청구범위 4에 따른 방법.
  6. 다음 일반식으로 표시되는 중격화합물
    (여기서 R1,R2,R3,R4,R6와 R7은 청구범위 1에 언급된 바와 같고, Q는 히드록실, 티올 또는 아미노이다).
  7. 다음 일반식으로 표시되는 중간화합물
    (여기서 R1에서 R7까지는 청구범위 1에 언급된 바와 같다)
    ※ 참고사항 : 최초출S원 내용에 의하여 공개하는 것임.
KR1019800003960A 1979-10-16 1980-10-15 벤조디아제핀 화합물의 제조 방법 KR850000471B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019840004388A KR850000472B1 (ko) 1979-10-16 1984-07-24 벤조디아제핀 화합물의 제조방법

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GB7935846 1977-10-16
GB7935846 1979-10-16

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KR1019840004388A Division KR850000472B1 (ko) 1979-10-16 1984-07-24 벤조디아제핀 화합물의 제조방법

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KR830004300A true KR830004300A (ko) 1983-07-09
KR850000471B1 KR850000471B1 (ko) 1985-04-08

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KR1019800003960A KR850000471B1 (ko) 1979-10-16 1980-10-15 벤조디아제핀 화합물의 제조 방법
KR1019840004388A KR850000472B1 (ko) 1979-10-16 1984-07-24 벤조디아제핀 화합물의 제조방법

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Country Status (33)

Country Link
US (3) US4404137A (ko)
EP (1) EP0027390B1 (ko)
JP (1) JPS5663987A (ko)
KR (2) KR850000471B1 (ko)
AR (2) AR228041A1 (ko)
AT (1) AT373889B (ko)
AU (1) AU538500B2 (ko)
BE (1) BE885729A (ko)
BG (2) BG34907A3 (ko)
CA (1) CA1159056A (ko)
CH (1) CH646700A5 (ko)
CS (1) CS244409B2 (ko)
DD (1) DD153692A5 (ko)
DE (1) DE3068706D1 (ko)
DK (1) DK437480A (ko)
ES (1) ES495948A0 (ko)
FI (1) FI67550C (ko)
FR (1) FR2467851A1 (ko)
GB (1) GB8327127D0 (ko)
GR (1) GR70720B (ko)
HU (1) HU182213B (ko)
IE (1) IE50358B1 (ko)
IL (1) IL61264A (ko)
IT (1) IT1143047B (ko)
LU (1) LU82853A1 (ko)
MX (1) MX6233E (ko)
NZ (1) NZ195248A (ko)
PH (2) PH16288A (ko)
PL (2) PL135044B1 (ko)
PT (1) PT71913B (ko)
RO (2) RO85822B (ko)
YU (1) YU261580A (ko)
ZA (1) ZA806342B (ko)

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* Cited by examiner, † Cited by third party
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US4404137A (en) * 1979-10-16 1983-09-13 Lilly Industries Limited Pyrazolo [3,4-b][1,5]benzodiazepine compounds
US4431589A (en) * 1980-12-11 1984-02-14 Lilly House Benzodiazepine compounds and their use as pharmaceuticals
US4596799A (en) * 1985-01-29 1986-06-24 Ciba-Geigy Corporation 9H-pyrrolo[2,1-c]-1,2,4-triazolo[4,3-a][1,4]benzodiazepines
TW219896B (ko) * 1988-07-07 1994-02-01 Duphar Int Res
GB8819059D0 (en) * 1988-08-11 1988-09-14 Lilly Industries Ltd Benzodiazepine compounds & their use as pharmaceuticals
US5631250A (en) * 1995-03-24 1997-05-20 Eli Lilly And Company Process and solvate of 2-methyl-thieno-benzodiazepine
US5637584A (en) * 1995-03-24 1997-06-10 Eli Lilly And Company Solvate of olanzapine
MXPA05007784A (es) * 2003-01-23 2005-09-30 Acadia Pharm Inc Empleo de la n-desmetilclozapina para tratar las enfermedades neuropsiquiatricas humanas.
US20050250767A1 (en) * 2003-01-23 2005-11-10 Weiner David M Use of N-desmethylclozapine to treat human neuropsychiatric disease
US20050085463A1 (en) * 2003-01-23 2005-04-21 Weiner David M. Use of N-desmethylclozapine to treat human neuropsychiatric disease
PL1696931T3 (pl) * 2003-12-22 2009-10-30 Acadia Pharm Inc Aminopodstawione analogi diarylo[A,D]cykloheptenowe jako agoniści receptorów muskarynowych i sposoby leczenia chorób neuropsychiatrycznych
MXPA06011320A (es) * 2004-04-01 2007-03-21 Acadia Pharm Inc Metodo de sintesis y aislamiento de n-desmetilclozapina solida y sus formas cristalinas.
WO2007053618A1 (en) * 2005-10-31 2007-05-10 Acadia Pharmaceuticals Inc. Prodrugs of muscarinic agonists and methods of treatment of neuropsychiatric disorders
JP5438482B2 (ja) * 2009-12-03 2014-03-12 Ｊｕｋｉ株式会社 ミシン、ミシンの縫製データ編集装置及びミシンの縫製データ編集プログラム

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US3450694A (en) * 1966-02-23 1969-06-17 Abbott Lab Substituted benzoxazepines and benzothiazepines
US3758479A (en) * 1967-03-22 1973-09-11 Sandoz Ag Nitro and sulphamoyl substituted dibenzodiazepines
DE1795183B1 (de) * 1968-08-20 1972-07-20 Thomae Gmbh Dr K 5,11-Dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-on-derivate und Arzneimittel
CA918659A (en) * 1969-07-31 1973-01-09 Yoshitomi Pharmaceutical Industries 11-(4-substituted-1-piperazinyl)-dibenzo (b,f) (1,4) thiazepines
US4172831A (en) * 1974-11-26 1979-10-30 Lilly Industries Limited Thieno-benzodiazepines
US4115568A (en) * 1974-11-26 1978-09-19 Lilly Industries Limited Thieno[3,2-b]-[1,5]benzodiazepines
US3951981A (en) * 1975-02-24 1976-04-20 American Cyanamid Company Substituted benzodiazepines and method of use
US3953430A (en) * 1975-02-24 1976-04-27 American Cyanamid Company Substituted benzodiazepin-10-ones and method of use
DE2707269A1 (de) * 1977-02-19 1978-08-24 Hoechst Ag Heterocyclische stickstoffverbindungen und verfahren zu ihrer herstellung
DE2707270A1 (de) * 1977-02-19 1978-08-24 Hoechst Ag Pyrazolo-diazepine und verfahren zu ihrer herstellung
US4097597A (en) * 1977-02-23 1978-06-27 Abbott Laboratories Dibenzo b,e! 1,4!diazepines
IT7851496A0 (it) * 1977-10-31 1978-10-13 Sandoz Ag Menti pirazinobenzossazepine loro preparazione e loro impiego quali medica
CH643263A5 (de) * 1979-05-11 1984-05-30 Sandoz Ag Benzodiazepine, ihre herstellung und verwendung.
FI68835C (fi) * 1979-08-03 1985-11-11 Byk Gulden Lomberg Chem Fab Foerfarande foer framstaellning av terapeutiskt anvaendbara 4-minoacyl-1,4,9,10-tetrahydropyrazolo(4,3-b)(1,5)bensodiaz epn-10-oner
US4404137A (en) * 1979-10-16 1983-09-13 Lilly Industries Limited Pyrazolo [3,4-b][1,5]benzodiazepine compounds

Also Published As

Publication number Publication date
DD153692A5 (de) 1982-01-27
ZA806342B (en) 1982-05-26
IE50358B1 (en) 1986-04-02
KR850000471B1 (ko) 1985-04-08
RO81351A (ro) 1983-02-15
IT1143047B (it) 1986-10-22
CH646700A5 (fr) 1984-12-14
RO85822B (ro) 1984-11-30
YU261580A (en) 1983-12-31
US4486591A (en) 1984-12-04
PL126824B1 (en) 1983-09-30
KR850000472B1 (ko) 1985-04-08
PT71913B (en) 1981-08-31
PL231270A1 (ko) 1981-12-23
FR2467851A1 (fr) 1981-04-30
IE802135L (en) 1981-04-16
HU182213B (en) 1983-12-28
US4404137A (en) 1983-09-13
JPS5663987A (en) 1981-05-30
FI67550B (fi) 1984-12-31
KR850001463A (ko) 1985-03-18
CA1159056A (en) 1983-12-20
RO85822A (ro) 1984-11-25
IT8049899A0 (it) 1980-10-14
BG35042A3 (en) 1983-01-16
ES8106905A1 (es) 1981-09-16
EP0027390A1 (en) 1981-04-22
RO81351B (ro) 1983-02-28
PT71913A (en) 1980-11-01
LU82853A1 (fr) 1982-05-10
CS244409B2 (en) 1986-07-17
PL227306A1 (ko) 1981-09-18
BG34907A3 (en) 1983-12-15
MX6233E (es) 1985-01-14
ATA510180A (de) 1983-07-15
IL61264A0 (en) 1980-12-31
FI803253L (fi) 1981-04-17
AR228101A1 (es) 1983-01-14
BE885729A (fr) 1981-04-15
DE3068706D1 (en) 1984-08-30
PH17759A (en) 1984-12-05
EP0027390B1 (en) 1984-07-25
US4542131A (en) 1985-09-17
IL61264A (en) 1985-08-30
AU6325280A (en) 1981-04-30
PH16288A (en) 1983-09-05
AU538500B2 (en) 1984-08-16
FI67550C (fi) 1985-04-10
PL135044B1 (en) 1985-09-30
AT373889B (de) 1984-02-27
NZ195248A (en) 1983-11-18
GB8327127D0 (en) 1983-11-09
ES495948A0 (es) 1981-09-16
DK437480A (da) 1981-04-17
GR70720B (ko) 1983-01-18
AR228041A1 (es) 1983-01-14
FR2467851B1 (ko) 1985-04-05

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