KR101821090B1 - N-아실비페닐 알라닌의 제조 방법 - Google Patents

N-아실비페닐 알라닌의 제조 방법 Download PDF

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Publication number
KR101821090B1
KR101821090B1 KR1020167036201A KR20167036201A KR101821090B1 KR 101821090 B1 KR101821090 B1 KR 101821090B1 KR 1020167036201 A KR1020167036201 A KR 1020167036201A KR 20167036201 A KR20167036201 A KR 20167036201A KR 101821090 B1 KR101821090 B1 KR 101821090B1
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formula
compound
acid
methyl
salt
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Korean (ko)
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KR20170002681A (ko
Inventor
구오리앙 주
더쑹 스
쥔후이 웨이
펑펑 타오
Original Assignee
제지앙 지우조우 파마슈티칼 컴퍼니 리미티드
노파르티스 아게
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Priority claimed from PCT/CN2009/074125 external-priority patent/WO2010034236A1/en
Application filed by 제지앙 지우조우 파마슈티칼 컴퍼니 리미티드, 노파르티스 아게 filed Critical 제지앙 지우조우 파마슈티칼 컴퍼니 리미티드
Publication of KR20170002681A publication Critical patent/KR20170002681A/ko
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/51Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/83Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/82Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/87Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18Oxygen atoms
    • C07D263/20Oxygen atoms attached in position 2

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
KR1020167036201A 2009-09-23 2010-03-23 N-아실비페닐 알라닌의 제조 방법 Expired - Fee Related KR101821090B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2009/074125 2009-09-23
PCT/CN2009/074125 WO2010034236A1 (en) 2008-09-24 2009-09-23 Process for the manufacture of n-acylbiphenyl alanine
PCT/CN2010/071243 WO2011035569A1 (en) 2009-09-23 2010-03-23 Process for manufacture of n-acylbphenyl alanine

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020127010180A Division KR20120093227A (ko) 2009-09-23 2010-03-23 N-아실비페닐 알라닌의 제조 방법

Publications (2)

Publication Number Publication Date
KR20170002681A KR20170002681A (ko) 2017-01-06
KR101821090B1 true KR101821090B1 (ko) 2018-01-22

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KR1020167036201A Expired - Fee Related KR101821090B1 (ko) 2009-09-23 2010-03-23 N-아실비페닐 알라닌의 제조 방법
KR1020127010180A Ceased KR20120093227A (ko) 2009-09-23 2010-03-23 N-아실비페닐 알라닌의 제조 방법

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KR1020127010180A Ceased KR20120093227A (ko) 2009-09-23 2010-03-23 N-아실비페닐 알라닌의 제조 방법

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Country Link
US (1) US20160115118A1 (enExample)
EP (1) EP2480523B1 (enExample)
JP (1) JP5894531B2 (enExample)
KR (2) KR101821090B1 (enExample)
CN (1) CN102639486B (enExample)
AU (1) AU2010297892B2 (enExample)
BR (1) BR112012006406A2 (enExample)
CA (1) CA2772681C (enExample)
IN (1) IN2012DN01968A (enExample)
RU (1) RU2534619C2 (enExample)
WO (1) WO2011035569A1 (enExample)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201101672A1 (ru) 2009-05-28 2012-06-29 Новартис Аг Замещенные производные аминомасляной кислоты в качестве ингибиторов неприлизина
JP5420761B2 (ja) 2009-05-28 2014-02-19 ノバルティス アーゲー ネプリリシン阻害剤としての置換アミノプロピオン酸誘導体
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
KR20150119107A (ko) 2013-02-14 2015-10-23 노파르티스 아게 개선된 생체내 효능을 갖는 nep 억제제로서의 치환된 비스페닐 부탄산 유도체
EP2956464B1 (en) 2013-02-14 2018-03-28 Novartis AG Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors
TW201632493A (zh) 2015-02-13 2016-09-16 諾華公司 新穎方法
WO2017051326A1 (en) 2015-09-23 2017-03-30 Novartis Ag New processes and intermediates useful in synthesis of nep inhibitors
JO3771B1 (ar) 2015-12-10 2021-01-31 Novartis Ag متوسطات لتحضير ساكوبيتريل وتحضيرها
JP6944473B2 (ja) 2016-07-05 2021-10-06 ノバルティス アーゲー 初期サクビトリル中間体のための新規な方法
WO2018033866A1 (en) 2016-08-17 2018-02-22 Novartis Ag New processes and intermediates for nep inhibitor synthesis
CN107778192A (zh) * 2016-08-26 2018-03-09 浙江九洲药业股份有限公司 一种n‑烷氧或苄氧羰基手性氨酸的制备方法
EP3558930B1 (en) 2016-12-23 2021-05-26 Novartis AG New process for early sacubitril intermediates
UY38072A (es) 2018-02-07 2019-10-01 Novartis Ag Compuestos derivados de éster butanoico sustituido con bisfenilo como inhibidores de nep, composiciones y combinaciones de los mismos

Citations (3)

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JP2001523240A (ja) * 1997-04-24 2001-11-20 アクゾ・ノベル・エヌ・ベー ヘテロ環誘導体および抗血栓剤としてのその使用
US20040180943A1 (en) * 2002-07-23 2004-09-16 Augelli-Szafran Corinne Elizabeth Oxazolone analogs as amyloid aggregation inhibitors and for the treatment of alzheimer's disease and disorders related to amyloidosis
JP2006504643A (ja) * 2002-07-01 2006-02-09 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー Hcvns5bポリメラーゼ阻害剤

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JPS60185752A (ja) * 1984-03-05 1985-09-21 Mitsui Toatsu Chem Inc α−アセトアミド桂皮酸類の製造法
JPS60215657A (ja) * 1984-04-10 1985-10-29 Mitsui Toatsu Chem Inc N−アシルフエニルアラニン類の製造法
JPS6245554A (ja) * 1985-08-23 1987-02-27 Nippon Redarii Kk 4−ビフエニリル酢酸の簡易製造法
CA1325222C (en) * 1985-08-23 1993-12-14 Lederle (Japan), Ltd. Process for producing 4-biphenylylacetic acid
FR2662440B1 (fr) * 1990-05-22 1992-07-31 Rhone Poulenc Sante Procede de preparation stereoselective de derives de la phenylisoserine.
GB2354440A (en) * 1999-07-20 2001-03-28 Merck & Co Inc Aryl amides as cell adhesion inhibitors
JP4270484B2 (ja) * 2002-03-08 2009-06-03 第一ファインケミカル株式会社 光学活性フェニルアラニン誘導体の製造方法
AR070176A1 (es) 2008-01-17 2010-03-17 Novartis Ag Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis
CN101684077B (zh) * 2008-09-24 2013-01-02 浙江九洲药业股份有限公司 N-酰基联苯丙氨酸的制备方法
CN101774941A (zh) * 2009-01-13 2010-07-14 浙江九洲药业股份有限公司 2-酰基氨基-3-联苯基丙酸的制备及拆分方法
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Publication number Priority date Publication date Assignee Title
JP2001523240A (ja) * 1997-04-24 2001-11-20 アクゾ・ノベル・エヌ・ベー ヘテロ環誘導体および抗血栓剤としてのその使用
JP2006504643A (ja) * 2002-07-01 2006-02-09 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー Hcvns5bポリメラーゼ阻害剤
US20040180943A1 (en) * 2002-07-23 2004-09-16 Augelli-Szafran Corinne Elizabeth Oxazolone analogs as amyloid aggregation inhibitors and for the treatment of alzheimer's disease and disorders related to amyloidosis

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CN102639486A (zh) 2012-08-15
JP5894531B2 (ja) 2016-03-30
EP2480523A4 (en) 2013-06-26
KR20120093227A (ko) 2012-08-22
RU2012116208A (ru) 2013-11-10
AU2010297892B2 (en) 2014-02-06
BR112012006406A2 (pt) 2016-04-12
EP2480523B1 (en) 2017-03-01
IN2012DN01968A (enExample) 2015-08-21
CA2772681A1 (en) 2011-03-31
CA2772681C (en) 2017-01-03
CN102639486B (zh) 2014-12-31
RU2534619C2 (ru) 2014-11-27
KR20170002681A (ko) 2017-01-06
JP2013505273A (ja) 2013-02-14
US20160115118A1 (en) 2016-04-28
AU2010297892A1 (en) 2012-03-22
WO2011035569A1 (en) 2011-03-31
EP2480523A1 (en) 2012-08-01

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