KR830007556A - 2-아미노-3-카브에톡시아민노-6-(p-플루오로-벤질아미노)-피리딘-말레에이트의 제조방법 - Google Patents

2-아미노-3-카브에톡시아민노-6-(p-플루오로-벤질아미노)-피리딘-말레에이트의 제조방법 Download PDF

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KR830007556A
KR830007556A KR1019810003406A KR810003406A KR830007556A KR 830007556 A KR830007556 A KR 830007556A KR 1019810003406 A KR1019810003406 A KR 1019810003406A KR 810003406 A KR810003406 A KR 810003406A KR 830007556 A KR830007556 A KR 830007556A
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pyridine
maleate
benzylamino
fluoro
amino
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KR1019810003406A
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KR860000585B1 (ko
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폰 베벤부르크 발터
파울룬 지그프리트
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도이체 골트-운트 질베르-샤이데안스탈트 포르말스 뢰슬러 아크티엔 게젤샤프트
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/76—Nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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

Abstract

내용 없음

Description

2-아미노-3-카브에톡시아민노-6-(p-플루오로-벤질아미노)-피리딘-말레에이트의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도(Y,II)는 결정변형 A가 보강된(함량 60 내지 90%) 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노-피리딘 유리염기의 IR(KBr내)스펙트럼을 나타낸다

Claims (7)

1몰의 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리단을 용매내, 20℃ 내지 용매의 비점사이에서 1,1 내지 1.5물의 말레산과 반응시킴을 특징으로 하여 다음 일반식의 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리딘-말레에이트를 제조하는 방법.
제1항에 있어서 온도가 20℃ 내지 60℃인 방법.
제1항에 있어서 말레에이트 형성시에, 정제하기 위해 활성탄으로 처리된 불순한 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리딘의 말레에이트를 사용하며 이 불순한 피리딘의 융점은 117 내지 120℃인 방법.
제2항에 있어서 말레에이트가 석출되면 용매존재하에 30℃ 내지 용매의 비절의 온도범위내에서 5 재지 180분간 가열하는 방법.
제4항에 있어서 말레에이트 형성시에, 정제하기 위해 활성만으로 처리한 불순한 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리딘의 말레에이트를 사용하며 이 불순한 피리딘의 융점은 117 내ㅈ 120℃인 방법.
제5항에 있어서, 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리딘과 말레산의 반응을 20 내지 60℃에서, 용해되지 않은 접종결정 존재하에 수행하는 방법.
제4항에 있어서 2-아미노-3-카브에톡시아미노-6-(p-플루오로-벤질아미노)-피리딘과 말레산의 반응을 20 내지 60℃에서, 용해되지 않는 접종결정 존재하에 수행하는 방법.
※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019810003406A 1980-09-13 1981-09-11 2-아미노-3-카브에톡시아미노-6-(p-플루오로벤질아미노)-피리딘-말리에이트의 제조방법 KR860000585B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP3034638.4 1980-09-13
DE3034638 1980-09-13

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KR830007556A true KR830007556A (ko) 1983-10-21
KR860000585B1 KR860000585B1 (ko) 1986-05-17

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US (1) US4481205A (ko)
JP (1) JPS5781465A (ko)
KR (1) KR860000585B1 (ko)
AR (1) AR229101A1 (ko)
AT (1) AT375924B (ko)
AU (1) AU541020B2 (ko)
BE (1) BE890331A (ko)
CA (1) CA1147736A (ko)
CH (1) CH646952A5 (ko)
CS (1) CS226037B2 (ko)
DD (1) DD201786A5 (ko)
DK (1) DK159878C (ko)
EG (1) EG15446A (ko)
ES (1) ES505423A0 (ko)
FI (1) FI79531C (ko)
FR (1) FR2490225B1 (ko)
GB (1) GB2084138B (ko)
GR (1) GR75777B (ko)
HU (1) HU182720B (ko)
IE (1) IE51547B1 (ko)
IL (1) IL63801A (ko)
IN (1) IN155674B (ko)
IT (1) IT1171520B (ko)
LU (1) LU83633A1 (ko)
NL (1) NL189856C (ko)
NO (1) NO160919C (ko)
PL (1) PL130030B1 (ko)
SE (1) SE454693B (ko)
SU (1) SU1091855A3 (ko)
YU (1) YU43037B (ko)
ZA (1) ZA816336B (ko)

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DE3416609A1 (de) * 1984-05-05 1985-11-07 Degussa Ag, 6000 Frankfurt 2-amino-3-ethoxycarbonylamino-6-(p-fluor-benzylamino)- pyridin-gluconat und pharmazeutische zubereitungen, die diese substanz enthalten
NO860825L (no) * 1985-03-23 1986-09-24 Degussa Fremgangsmaate til fremstilling av 2-amino-3-nitro-6-(4-fluor-benzylamino)-pyridin samt 2-amino-3-karbetoksyamino-6-(4-fluor-benzylamino)-pyridin.
JPH0568848U (ja) * 1991-11-18 1993-09-17 京都機械工具株式会社 チューブ絞り器
DE4327516A1 (de) * 1993-08-17 1995-02-23 Asta Medica Ag Primäre und sekundäre neuroprotektive Wirkung bei neurodegenerativen Erkrankungen von Flupirtin
DE19625582A1 (de) * 1996-06-27 1998-01-02 Asta Medica Ag Verwendung von Flupirtin zur Prophylaxe und Therapie von Erkrankungen die mit einer unphysiologisch hohen Zellsterberate einhergehen
DE19716984A1 (de) * 1997-04-23 1998-10-29 Asta Medica Ag Verfahren zur Herstellung von reinem Flupirtin-Maleat und dessen Modifikation A
US6187324B1 (en) * 1998-08-11 2001-02-13 Kabushiki Kaisha Ogi Kogei Cosmetic composition comprising at least one of Kumazasa extract and medicinal carbon
US6821995B1 (en) 1999-12-01 2004-11-23 Duke University Method of treating batten disease
DE10327674A1 (de) * 2003-06-20 2005-01-05 Awd.Pharma Gmbh & Co. Kg Injizierbare Darreichungsform von Flupirtin
US7741358B2 (en) * 2005-04-14 2010-06-22 N.V. Organon Crystal form of asenapine maleate
US20080279930A1 (en) * 2007-05-07 2008-11-13 Bernd Terhaag Controlled-Release Flupirtine Compositions, Compacts, Kits and Methods of Making and Use Thereof
US8501778B2 (en) 2008-06-20 2013-08-06 Nhwa Pharma. Corporation Aralkyl piperidine derivatives and their uses as antalgic or ataractic agent
BRPI0916889A2 (pt) * 2008-08-06 2016-02-10 Bionevia Pharmaceuticals Inc composto, composição farmacêutica, e, métodos para tratar dor, para tratar um distúrbio ou uma doença, e para fabricar um co-cristal
DE102009023162B4 (de) * 2009-05-29 2011-07-07 Corden PharmaChem GmbH, 68305 Verfahren zur Herstellung von Flupirtin
CN102140077A (zh) * 2010-01-28 2011-08-03 范扶民 氟吡汀a晶型及其制备方法
WO2012004391A1 (en) 2010-07-09 2012-01-12 K.H.S. Pharma Holding Gmbh Process for the preparation of flupirtine maleate
CN102241626B (zh) * 2011-05-03 2013-07-03 北京华睿鼎信科技有限公司 一种马来酸氟吡汀的合成工艺
WO2013080215A1 (en) 2011-11-30 2013-06-06 Arch Pharmalabs Limited An improved process for the preparation of flupirtine and pharmaceutically acceptable salts thereof
CN103086963A (zh) * 2013-01-29 2013-05-08 吉林修正药业新药开发有限公司 一种马来酸氟吡汀a晶型化合物及中间体的合成方法
CN104086481B (zh) * 2014-07-18 2016-05-11 四川新斯顿制药股份有限公司 一种马来酸氟吡汀的合成方法
CN111100010A (zh) * 2019-12-30 2020-05-05 山东省越兴化工有限公司 一种对氟苄胺的制备方法

Family Cites Families (2)

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DE1795858C2 (de) * 1968-07-19 1979-01-11 Deutsche Gold- Und Silber-Scheideanstalt Vormals Roessler, 6000 Frankfurt Benzylaminopyridine
US3969361A (en) * 1972-05-10 1976-07-13 Deutsche Gold- Und Silber-Scheideanstalt Vormals Roessler 2-Benzoyl-3-amino-pyridines

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GR75777B (ko) 1984-08-02
FI812836L (fi) 1982-03-14
FR2490225B1 (fr) 1985-09-06
IT1171520B (it) 1987-06-10
DD201786A5 (de) 1983-08-10
AR229101A1 (es) 1983-06-15
CS226037B2 (en) 1984-03-19
IE812055L (en) 1982-03-13
FI79531B (fi) 1989-09-29
KR860000585B1 (ko) 1986-05-17
JPH0259149B2 (ko) 1990-12-11
BE890331A (fr) 1982-03-11
NO160919C (no) 1989-06-14
FR2490225A1 (fr) 1982-03-19
IL63801A0 (en) 1981-12-31
US4481205A (en) 1984-11-06
GB2084138B (en) 1984-07-25
NL189856B (nl) 1993-03-16
ES8206481A1 (es) 1982-08-16
SU1091855A3 (ru) 1984-05-07
FI79531C (fi) 1990-01-10
ZA816336B (en) 1982-09-29
HU182720B (en) 1984-03-28
AU7516381A (en) 1982-03-25
IT8149272A0 (it) 1981-09-11
SE8105425L (sv) 1982-03-14
CH646952A5 (de) 1984-12-28
PL130030B1 (en) 1984-07-31
PL232999A1 (ko) 1982-08-16
NO813082L (no) 1982-03-15
DK159878C (da) 1991-05-13
YU215781A (en) 1984-02-29
DK404681A (da) 1982-03-14
NL8104211A (nl) 1982-04-01
LU83633A1 (de) 1982-01-21
NO160919B (no) 1989-03-06
IN155674B (ko) 1985-02-23
DK159878B (da) 1990-12-24
ES505423A0 (es) 1982-08-16
CA1147736A (en) 1983-06-07
GB2084138A (en) 1982-04-07
IE51547B1 (en) 1987-01-07
YU43037B (en) 1989-02-28
IL63801A (en) 1984-10-31
AT375924B (de) 1984-09-25
AU541020B2 (en) 1984-12-13
EG15446A (en) 1986-06-30
NL189856C (nl) 1993-08-16
SE454693B (sv) 1988-05-24
JPS5781465A (en) 1982-05-21
ATA393481A (de) 1984-02-15

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