WO2010036048A3 - 몬테루카스트 나트륨염의 제조방법 - Google Patents

몬테루카스트 나트륨염의 제조방법 Download PDF

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Publication number
WO2010036048A3
WO2010036048A3 PCT/KR2009/005472 KR2009005472W WO2010036048A3 WO 2010036048 A3 WO2010036048 A3 WO 2010036048A3 KR 2009005472 W KR2009005472 W KR 2009005472W WO 2010036048 A3 WO2010036048 A3 WO 2010036048A3
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WO
WIPO (PCT)
Prior art keywords
chemical formula
sodium salts
compound
salts
montelukast sodium
Prior art date
Application number
PCT/KR2009/005472
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English (en)
French (fr)
Other versions
WO2010036048A2 (ko
Inventor
이인상
이석주
강재은
Original Assignee
주식회사 엘지생명과학
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 주식회사 엘지생명과학 filed Critical 주식회사 엘지생명과학
Priority to BRPI0914185-5A priority Critical patent/BRPI0914185A2/pt
Priority to CN200980138227XA priority patent/CN102164897B/zh
Priority to JP2011528936A priority patent/JP5531018B2/ja
Priority to US13/062,353 priority patent/US8426600B2/en
Publication of WO2010036048A2 publication Critical patent/WO2010036048A2/ko
Publication of WO2010036048A3 publication Critical patent/WO2010036048A3/ko

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F1/00Compounds containing elements of Groups 1 or 11 of the Periodic System
    • C07F1/04Sodium compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/18Halogen atoms or nitro radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Pulmonology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Quinoline Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 명세서 내의 화학식 1의 몬테루카스트 나트륨염을 제조하는 방법으로서, 화학식 2의 메탄설포닐 화합물과 화학식 3의 화합물을 비스트리메틸실릴아미드알칼리금속염 존재 하에 커플링 반응시킨 후 알칼리 금속 염기를 추가로 투입하고 가열하여 가수분해시킴으로써 화학식 4의 화합물을 제조하고, 이를 4-tert-부틸시클로헥실아민과 반응시킨 후 정제하여 화학식 5의 아민염을 제조한 다음, 상기 아민염을 나트륨염으로 변환시키는 과정을 포함하는 제조방법을 제공한다.
PCT/KR2009/005472 2008-09-26 2009-09-25 몬테루카스트 나트륨염의 제조방법 WO2010036048A2 (ko)

Priority Applications (4)

Application Number Priority Date Filing Date Title
BRPI0914185-5A BRPI0914185A2 (pt) 2008-09-26 2009-09-25 Método para preparar sais de montelucaste de sódio
CN200980138227XA CN102164897B (zh) 2008-09-26 2009-09-25 制备孟鲁司特钠盐的方法
JP2011528936A JP5531018B2 (ja) 2008-09-26 2009-09-25 モンテルカストナトリウム塩の製造方法
US13/062,353 US8426600B2 (en) 2008-09-26 2009-09-25 Method for preparing montelukast sodium salts

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2008-0094731 2008-09-26
KR20080094731 2008-09-26

Publications (2)

Publication Number Publication Date
WO2010036048A2 WO2010036048A2 (ko) 2010-04-01
WO2010036048A3 true WO2010036048A3 (ko) 2010-08-19

Family

ID=42060289

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2009/005472 WO2010036048A2 (ko) 2008-09-26 2009-09-25 몬테루카스트 나트륨염의 제조방법

Country Status (6)

Country Link
US (1) US8426600B2 (ko)
JP (1) JP5531018B2 (ko)
KR (1) KR101123292B1 (ko)
CN (1) CN102164897B (ko)
BR (1) BRPI0914185A2 (ko)
WO (1) WO2010036048A2 (ko)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100990046B1 (ko) * 2010-07-30 2010-10-26 동국제약 주식회사 신규한 몬테루카스트 4-할로 벤질아민염 및 이를 이용한 몬테루카스트 나트륨염의 제조방법
KR20130041664A (ko) * 2011-10-17 2013-04-25 주식회사 엘지생명과학 고순도 몬테루카스트 나트륨 염의 제조 방법
CN104055741B (zh) * 2013-03-18 2017-02-15 青岛大学 一种孟鲁司特钠片剂及其制备方法
CN103570618A (zh) * 2013-09-30 2014-02-12 浙江车头制药股份有限公司 一种孟鲁司特钠盐的制备方法
CN105622500B (zh) * 2016-02-29 2018-03-02 山东新时代药业有限公司 孟鲁司特钠中间体的制备方法
JP2021536467A (ja) 2018-09-06 2021-12-27 インノファーマスクリーン インコーポレイテッド 喘息またはパーキンソン病の処置のための方法および組成物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105751A1 (en) * 2004-04-21 2005-11-10 Teva Pharmaceutical Industries Ltd. Processes for preparing montelukast sodium
WO2006064269A2 (en) * 2004-12-17 2006-06-22 Cipla Limited Salts of leukotriene antagonist montelukast
US20070208178A1 (en) * 2006-02-27 2007-09-06 Chemagis Ltd. Process for preparing montelukast and salts thereof
WO2008017669A1 (en) * 2006-08-09 2008-02-14 Esteve Química, S. A. Purification process of montelukast and its amine salts
WO2008072872A1 (en) * 2006-12-14 2008-06-19 Hanmi Pharm. Co., Ltd. Method of preparing montelukast and intermediates used therein

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0480717T3 (da) 1990-10-12 1999-02-08 Merck Frosst Canada Inc Umættede hydroxyalkylquinolinsyrer som leukotrienantagonister
TW416948B (en) * 1993-12-28 2001-01-01 Merck & Co Inc Process for the preparation of leukotriene antagonists
US6716452B1 (en) * 2000-08-22 2004-04-06 New River Pharmaceuticals Inc. Active agent delivery systems and methods for protecting and administering active agents
EP1708708A1 (en) * 2004-01-30 2006-10-11 Teva Pharmaceutical Industries Ltd. Montelukast free acid polymorphs
EP1812394B1 (en) 2004-07-19 2011-03-02 Matrix Laboratories Ltd Process for the preparation of montelukast and its salts
PL205637B1 (pl) * 2004-10-22 2010-05-31 Inst Farmaceutyczny Sposób wytwarzania kwasu (R,E)-(1-{1-{3-[2-(7-chlorochinolin-2-ylo)etenylo]fenylo}-3-[2-(1-hydroksy-1-metyloetylo)fenylo] propylosulfanylometylo}cyklopropylo)octowego i/lub jego farmaceutycznie dopuszczalnych soli
US8252806B2 (en) * 2005-03-14 2012-08-28 Neurosearch A/S Potassium channel modulating agents and their medical use
EP1940793A4 (en) * 2005-07-05 2011-03-23 Matrix Lab Ltd METHOD FOR PRODUCING MONTELUCASTS
ES2403067T3 (es) * 2005-12-13 2013-05-13 Msn Laboratories Limited Un procedimiento mejorado para la preparación de montelukast y sus sales farmaceúticamente aceptables
WO2008023044A1 (en) * 2006-08-23 2008-02-28 Sandoz Ag Process for the preparation of montelukast free acid and its amine salts
US8115004B2 (en) 2006-11-20 2012-02-14 Msn Laboratories Limited Process for pure montelukast sodium through pure intermediates as well as amine salts
WO2008087628A1 (en) * 2007-01-15 2008-07-24 Chemagis Ltd. Process for preparing montelukast sodium containing controlled levels of impurities
KR101469015B1 (ko) * 2008-02-25 2014-12-05 주식회사 종근당 몬테루카스트의 제조방법 및 이에 사용되는 중간체

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105751A1 (en) * 2004-04-21 2005-11-10 Teva Pharmaceutical Industries Ltd. Processes for preparing montelukast sodium
WO2006064269A2 (en) * 2004-12-17 2006-06-22 Cipla Limited Salts of leukotriene antagonist montelukast
US20070208178A1 (en) * 2006-02-27 2007-09-06 Chemagis Ltd. Process for preparing montelukast and salts thereof
WO2008017669A1 (en) * 2006-08-09 2008-02-14 Esteve Química, S. A. Purification process of montelukast and its amine salts
WO2008072872A1 (en) * 2006-12-14 2008-06-19 Hanmi Pharm. Co., Ltd. Method of preparing montelukast and intermediates used therein

Also Published As

Publication number Publication date
CN102164897B (zh) 2013-04-17
US20110166356A1 (en) 2011-07-07
JP2012503648A (ja) 2012-02-09
JP5531018B2 (ja) 2014-06-25
US8426600B2 (en) 2013-04-23
BRPI0914185A2 (pt) 2015-08-04
WO2010036048A2 (ko) 2010-04-01
CN102164897A (zh) 2011-08-24
KR20100035597A (ko) 2010-04-05
KR101123292B1 (ko) 2012-03-19

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