KR870002053A - P-아실아미노벤즈아미드의 제조 방법 - Google Patents

P-아실아미노벤즈아미드의 제조 방법 Download PDF

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KR870002053A
KR870002053A KR1019860007213A KR860007213A KR870002053A KR 870002053 A KR870002053 A KR 870002053A KR 1019860007213 A KR1019860007213 A KR 1019860007213A KR 860007213 A KR860007213 A KR 860007213A KR 870002053 A KR870002053 A KR 870002053A
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South Korea
Prior art keywords
alkyl
benzamide
dimethylphenyl
pharmaceutically acceptable
acid addition
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KR1019860007213A
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KR900000275B1 (ko
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웨인 로버트슨 데이비드
얼 비들 에드워드
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메리 앤 터커
일라이 릴리 앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

내용 없음.

Description

P-아실아미노벤즈아미드의 제조 방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. a) 일반식 (IV)의 화합물을 일반식이인 아실화제(여기서, Ra는 C1내지 C6의 알킬 또는 C3내지 C7의 사이클로알킬이며, X는 브로모, 클로로, -OH 또는 -OCORa이다)로 아실화하거나, b) 일반식 (II)의 화합물을 일반식이 R8R9NH인 아민(여기서, R8및 R9는 각각 독립적으로 수소, C1내지 C6의 알킬 또는 C3내지 C7의 사이클로알킬이거나, 질소원자와 함께 결합되어 피롤리디노, 피페리디노, 호모피페리디노, 모르폴리노 또는 N-메틸피페라지노를 형성하며, “alk”는 C1내지 C6의 지방족 탄화수소로 부터 유도된 2가의 유기 라디칼이다)과 반응시키고, 임의로 생성물의 약제학적으로 허용가능한산 부가염을 형성함을 특징으로 하여 일반식(I)의 화합물 또는 약제학적으로 허용가능한 이의 산 부가염을 제조하는 방법.
    상기식에서, R1은 C1내지 C6의 알킬, C3내지 C7의 알킬 또는 R8R9N-alk-(여기서, R8및 R9는 각각 독립적으로 수소, C1내지 C6의 알킬 또는 C3내지 C7의 사이클로알킬이거나, 질소원자와 함께 결합되어 피롤리디노, 피페리디노, 호모피페리디노, 모르폴리노 또는 N-메틸-피페라지노를 형성하며, “alk”는 C1내지 C6의 지방족 탄화수소로부터 유도된 2가의 유기 라디칼이다)이고; R2,R3,R4,R5,R6및 R7은 각각 독립적으로 수소 또는 메틸이고; n은 0 또는 1이며; R1′는 브로모-또는 클로로-치환된 C1내지 C6의 알킬이다.
  2. 제1항에 있어서, 4-아미노-N-(2,6-디메틸페닐)벤즈아미드를 일반식이인 아실화제(여기서, Ra는 C1내지 C6의 알킬이며, X는 브로모, 클로로, -OH 또는 -OCORa이다)와 반응시킨 다음, 임의로 이의 생성물을 약제학적으로 허용가능한 산 부가염으로 전환시킴을 특징으로 하는 방법.
  3. 제2항에 있어서, 4-아미노-N-(2,6-디메틸페닐)벤즈아미드를 아세틸 클로라이드와 반응시켜 4-(아세틸아미노)-N-(2,6-디메틸페닐)벤즈아미드를 제조한 다음, 임의로 이의 생성물을 약제학적으로 허용가능한 산 부가염으로 전환시킴을 특징으로 하는 방법.
  4. 제1항에 있어서, 4-[(클로로아세틸)아미노]-N-(2,6-디메틸페닐)벤즈아미드를 일반식이 R8R9NH인 아민(여기서, R8및 R9는 제1항에서 정의한 바와 같다)과 반응시킨 다음, 임의로 이의 생성물을 약제학적으로 허용가능한 산 부가염으로 전환시킴을 특징으로 하는 방법.
  5. 제4항에 있어서, 4-[(클로로아세틸)아미노]-N-(2,6-디메틸페닐)벤즈아미드를 디에틸아민과 반응시켜 4-([(디에틸아미노)아세틸]아미노)-N-(2,6-디메틸페닐)벤즈아미드를 제조한 다음, 임의로 이의 생성물을 약제학적으로 허용가능한 산 부가염으로 전환시킴을 특징으로 하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019860007213A 1985-08-30 1986-08-29 P-아실아미노벤즈아미드 및 이의 제조방법 KR900000275B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US771455 1985-08-30
US06/771,455 US4642379A (en) 1985-08-30 1985-08-30 Intermediates for anticonvulsant agents

Publications (2)

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KR870002053A true KR870002053A (ko) 1987-03-28
KR900000275B1 KR900000275B1 (ko) 1990-01-24

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Country Status (17)

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US (1) US4642379A (ko)
EP (1) EP0213924B1 (ko)
JP (1) JPS6259249A (ko)
KR (1) KR900000275B1 (ko)
CN (1) CN1010680B (ko)
AT (1) ATE57526T1 (ko)
AU (1) AU580890B2 (ko)
DE (1) DE3674971D1 (ko)
DK (1) DK412286A (ko)
ES (1) ES2001411A6 (ko)
HU (1) HU197029B (ko)
IL (1) IL79835A0 (ko)
NZ (1) NZ217356A (ko)
PH (1) PH23173A (ko)
PT (1) PT83253B (ko)
SU (1) SU1486055A3 (ko)
ZA (1) ZA866429B (ko)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ219974A (en) * 1986-04-22 1989-08-29 Goedecke Ag N-(2'-aminophenyl)-benzamide derivatives, process for their preparation and their use in the control of neoplastic diseases
US4835181A (en) * 1987-02-18 1989-05-30 Eli Lilly And Company Anticonvulsant agents using cyano dimethylphenyl benzamides
US4939163A (en) * 1987-02-18 1990-07-03 Eli Lilly And Company Anticonvulsant agents
US4981866A (en) * 1987-02-18 1991-01-01 Eli Lilly And Company Anticonvulsant agents
CA2252583A1 (en) * 1996-05-14 1997-11-20 Brett T. Watson Anticonvulsant pyridinyl benzamide derivatives
CA2695071A1 (en) * 2007-08-02 2009-02-05 F. Hoffmann-La Roche Ag The use of benzamide derivatives for the treatment of cns disorders

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2224153B1 (ko) * 1973-04-04 1977-11-10 Upjohn Co
US4004029A (en) * 1974-05-13 1977-01-18 The Upjohn Company Compositions and method for treating epilepsy and convulsions
JPS56156246A (en) * 1980-05-06 1981-12-02 Hodogaya Chem Co Ltd Benzamide derivative and herbicide comprising it
JPS5780351A (en) * 1980-11-06 1982-05-19 Hodogaya Chem Co Ltd Benzamide derivative and herbicide containing the same
US4379165A (en) * 1981-05-18 1983-04-05 Research Corporation Anti-convulsant
US4629740A (en) * 1984-04-10 1986-12-16 Eli Lilly And Company Anticonvulsant agents
US4835181A (en) * 1987-02-18 1989-05-30 Eli Lilly And Company Anticonvulsant agents using cyano dimethylphenyl benzamides

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AU580890B2 (en) 1989-02-02
US4642379A (en) 1987-02-10
ATE57526T1 (de) 1990-11-15
HU197029B (en) 1989-02-28
PH23173A (en) 1989-05-19
ZA866429B (en) 1988-04-27
JPS6259249A (ja) 1987-03-14
ES2001411A6 (es) 1988-05-16
IL79835A0 (en) 1986-11-30
KR900000275B1 (ko) 1990-01-24
CN86105906A (zh) 1987-02-25
EP0213924B1 (en) 1990-10-17
HUT41817A (en) 1987-05-28
DK412286D0 (da) 1986-08-29
AU6206486A (en) 1987-03-05
NZ217356A (en) 1989-05-29
PT83253A (en) 1986-09-01
DE3674971D1 (en) 1990-11-22
PT83253B (pt) 1989-03-30
SU1486055A3 (ru) 1989-06-07
EP0213924A2 (en) 1987-03-11
DK412286A (da) 1987-03-01
CN1010680B (zh) 1990-12-05
EP0213924A3 (en) 1987-09-30

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