KR840004428A - 벤조 아자시클로 알킬-스피로-이미다졸리딘의 제조방법 - Google Patents

벤조 아자시클로 알킬-스피로-이미다졸리딘의 제조방법 Download PDF

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KR840004428A
KR840004428A KR1019830001753A KR830001753A KR840004428A KR 840004428 A KR840004428 A KR 840004428A KR 1019830001753 A KR1019830001753 A KR 1019830001753A KR 830001753 A KR830001753 A KR 830001753A KR 840004428 A KR840004428 A KR 840004428A
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formula
hydrogen
spiro
carried out
acid
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KR1019830001753A
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말렝 찰스 (외 3)
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마리-샨딸 웬츠
아디르
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/38Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

내용 없음

Description

벤조 아자시클로 알킬-스피로-이미다졸리딘의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 다음 구조식(Ⅱ)의 케톤 유도체를 암모니움 산 또는 암모니움 염의 존재하에 알칼리 금속 시안화물과 축합시켜 다음 구조식(I´)의 스피로 히단토인을 얻고 필요하다면 R2가 수소인 다음 구조식(Ⅰ)의 화합물로 탈 벤질화 시키고 나머지를 저급 알카노인 산 할리드 또는 P-톨루엔 설포닐 할리드에 의해 아실화시켜 R2가 저급 알카노일 기 또는 P-톨루엔을 나타내는 구조식(Ⅰ)의 상응하는 화합물을 얻음을 특징으로 하는 다음 구조식(Ⅰ)의 벤조 아자시클로 알킬-스피로-이미다졸리딘 뿐만 아니라 약제학적으로 수용 가능한 무기 또는 유기 기재로 얻어지는 그것의 염 또는 약제학적으로 수용 가능한 무기산으로 얻어지는 그것의 염들(R2가 알카노일 또는 P-톨루엔 설포닐은 제외)의 제조방법.
    상기 구조식에서 R1은 수소나 할로겐 원자, 히드록시 또는 메톡시기를 나타내고 R2는 수소원자, 저급알킬기, 페닐저급-알킬기, 저급 알카닐기 또는 P-톨루엔 설포닐 기를 나타내고, n는 1 또는 2이고 R´2는 수소를 제외하고 상기한 R2의 의미와 같다.
  2. 상기 1항에 있어, 축합은 비점에서 극성용해중에 필요하다면 가압하에 암모니움 산 또는 암모니움염의 존재하에 수행됨을 특징으로 하는 상기의 제조방법.
  3. 상기 1항에 있어, 탈벤질화는 극성용매중 촉매 Pd/C의 존재하에 수행됨을 특징으로 하는 상기의 제조방법.
  4. 상기 1항에 있어, 아실화는 산수용체의 존재하에 수행됨을 특징으로 하는 상기의 제조방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019830001753A 1982-04-27 1983-04-26 벤조 아자시클로 알킬-스피로-이미다졸리딘의 제조방법 KR840004428A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR82.07203 1982-04-27
FR8207203A FR2525603A1 (fr) 1982-04-27 1982-04-27 Benzoazacycloalkyl-spiro-imidazolinines, leur preparation et leur application en therapeutique

Publications (1)

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KR840004428A true KR840004428A (ko) 1984-10-15

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KR1019830001753A KR840004428A (ko) 1982-04-27 1983-04-26 벤조 아자시클로 알킬-스피로-이미다졸리딘의 제조방법

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JP (1) JPS5910584A (ko)
KR (1) KR840004428A (ko)
AT (1) ATA125383A (ko)
AU (1) AU1395383A (ko)
BE (1) BE896572A (ko)
DD (1) DD209833A5 (ko)
DE (1) DE3315106A1 (ko)
DK (1) DK183583A (ko)
ES (1) ES521895A0 (ko)
FR (1) FR2525603A1 (ko)
GB (1) GB2133401B (ko)
GR (1) GR78481B (ko)
IL (1) IL68497A0 (ko)
IT (1) IT1167123B (ko)
LU (1) LU84770A1 (ko)
MA (1) MA19783A1 (ko)
NL (1) NL8301476A (ko)
NO (1) NO831473L (ko)
OA (1) OA07412A (ko)
PT (1) PT76595B (ko)
SE (1) SE8302347L (ko)
ZA (1) ZA832927B (ko)

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AU617541B2 (en) * 1988-10-20 1991-11-28 Wyeth Spiro-isoquinoline-pyrrolidine tetrones and analogs thereof useful as aldose reductase inhibitors
US4927831A (en) * 1988-10-20 1990-05-22 American Home Products Spiro-isoquinoline-pyrrolidine tetrones and analogs thereof useful as aldose reductase inhibitors
US6953787B2 (en) 2002-04-12 2005-10-11 Arena Pharmaceuticals, Inc. 5HT2C receptor modulators
EP2189448B1 (en) 2003-06-17 2014-01-29 Arena Pharmaceuticals, Inc. Processes for the Separation of 3-Benzazepine Racemates
CN101792417A (zh) 2003-06-17 2010-08-04 艾尼纳制药公司 用于治疗5ht2c受体相关疾病的苯并氮杂卓衍生物
KR101281919B1 (ko) 2004-12-21 2013-07-03 아레나 파마슈티칼스, 인크. (r)-8-클로로-1-메틸-2,3,4,5-테트라히드로-1h-3-벤즈아제핀 히드로클로라이드의 결정질 형태
PT1833473E (pt) 2004-12-23 2009-12-17 Arena Pharm Inc Composições de modulador de receptor 5ht2c e métodos de utilização
EP2001852A2 (en) 2006-04-03 2008-12-17 Arena Pharmaceuticals, Inc. Processes for the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates related thereto
CA2670285A1 (en) 2006-12-05 2008-06-12 Arena Pharmaceuticals, Inc. Processes for preparing (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine and intermediates thereof
JP5491421B2 (ja) 2008-03-04 2014-05-14 アリーナ ファーマシューティカルズ, インコーポレイテッド 5−ht2cアゴニストである(r)−8−クロロ−1−メチル−2,3,4,5−テトラヒドロ−1h−3−ベンゾアゼピンに関連する中間体の調製のためのプロセス
CN102648170A (zh) 2009-06-18 2012-08-22 艾尼纳制药公司 制备5-ht2c受体激动剂的方法
US9045431B2 (en) 2010-06-02 2015-06-02 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-HT2C receptor agonists
EP2939677A1 (en) 2010-09-01 2015-11-04 Arena Pharmaceuticals, Inc. Administration of lorcaserin to indviduals with renal impairment
CN103189360A (zh) 2010-09-01 2013-07-03 艾尼纳制药公司 5-ht2c激动剂的非吸湿性盐
ES2704455T3 (es) 2010-09-01 2019-03-18 Arena Pharm Inc Formas farmacéuticas de liberación modificada de agonistas de 5-HT2C útiles para la gestión del peso
WO2012030938A1 (en) 2010-09-01 2012-03-08 Arena Pharmaceuticals, Inc. Salts of lorcaserin with optically active acids
AU2012392187B2 (en) 2012-10-09 2018-07-12 Arena Pharmaceuticals, Inc. Method of weight management

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US4209630A (en) * 1976-10-18 1980-06-24 Pfizer Inc. Hydantoin derivatives as therapeutic agents
US4235911A (en) * 1979-06-13 1980-11-25 Pfizer Inc. Hydantoin derivatives

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ES8405796A1 (es) 1984-06-16
SE8302347L (sv) 1983-10-28
IT1167123B (it) 1987-05-13
ES521895A0 (es) 1984-06-16
GB2133401A (en) 1984-07-25
DK183583D0 (da) 1983-04-26
PT76595B (fr) 1986-01-21
DD209833A5 (de) 1984-05-23
ATA125383A (de) 1986-05-15
LU84770A1 (fr) 1984-11-28
JPS5910584A (ja) 1984-01-20
PT76595A (fr) 1983-05-01
SE8302347D0 (sv) 1983-04-26
IL68497A0 (en) 1983-07-31
OA07412A (fr) 1984-11-30
NL8301476A (nl) 1983-11-16
ZA832927B (en) 1984-06-27
AU1395383A (en) 1983-11-03
IT8348155A0 (it) 1983-04-26
NO831473L (no) 1983-10-28
FR2525603B1 (ko) 1984-09-14
GB8311508D0 (en) 1983-06-02
DK183583A (da) 1983-10-28
GB2133401B (en) 1985-10-23
BE896572A (fr) 1983-10-26
DE3315106A1 (de) 1983-11-03
GR78481B (ko) 1984-09-27
FR2525603A1 (fr) 1983-10-28
MA19783A1 (fr) 1983-12-31

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