CN102639486B - 生产n-酰基联苯基丙氨酸的方法 - Google Patents

生产n-酰基联苯基丙氨酸的方法 Download PDF

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Publication number
CN102639486B
CN102639486B CN201080042243.1A CN201080042243A CN102639486B CN 102639486 B CN102639486 B CN 102639486B CN 201080042243 A CN201080042243 A CN 201080042243A CN 102639486 B CN102639486 B CN 102639486B
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compound
formula
alkyl
salt
acid
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Chinese (zh)
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CN102639486A (zh
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朱国良
石德送
位军辉
陶峰峰
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Novartis AG
Ruibo Suzhou Pharmaceutical Co Ltd
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Novartis AG
Zhejiang Jiuzhou Pharmaceutical Co Ltd
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Priority claimed from PCT/CN2009/074125 external-priority patent/WO2010034236A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic 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
    • C07D263/16—Heterocyclic 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic 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
    • C07C233/46—Carboxylic 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
    • C07C233/47—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic 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
    • C07C233/46—Carboxylic 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
    • C07C233/51—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic 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
    • C07C233/82—Carboxylic 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
    • C07C233/83—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—Carboxylic 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
    • C07C233/82—Carboxylic 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
    • C07C233/87—Carboxylic 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

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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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN201080042243.1A 2009-09-23 2010-03-23 生产n-酰基联苯基丙氨酸的方法 Active CN102639486B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201080042243.1A CN102639486B (zh) 2009-09-23 2010-03-23 生产n-酰基联苯基丙氨酸的方法

Applications Claiming Priority (4)

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
CN201080042243.1A CN102639486B (zh) 2009-09-23 2010-03-23 生产n-酰基联苯基丙氨酸的方法
PCT/CN2010/071243 WO2011035569A1 (en) 2009-09-23 2010-03-23 Process for manufacture of n-acylbphenyl alanine

Publications (2)

Publication Number Publication Date
CN102639486A CN102639486A (zh) 2012-08-15
CN102639486B true CN102639486B (zh) 2014-12-31

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Country Status (11)

Country Link
US (1) US20160115118A1 (enExample)
EP (1) EP2480523B1 (enExample)
JP (1) JP5894531B2 (enExample)
KR (2) KR20120093227A (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
CN102448928B (zh) 2009-05-28 2014-10-01 诺华股份有限公司 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物
ES2602902T3 (es) 2009-05-28 2017-02-22 Novartis Ag Derivados aminopropiónicos sustituidos como inhibidores de neprilisina
JO2967B1 (en) 2009-11-20 2016-03-15 نوفارتس ايه جي Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors
TR201808541T4 (tr) 2013-02-14 2018-07-23 Novartis Ag Nep (nötr endopeptidaz) inhibitörleri olarak ikame edilmiş bisfenil butanoik fosfonik asit türevleri.
EP2956445A1 (en) 2013-02-14 2015-12-23 Novartis AG Substituted bisphenyl butanoic acid derivatives as nep inhibitors with improved in vivo efficacy
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
JP6945619B2 (ja) 2016-08-17 2021-10-06 ノバルティス アーゲー Ｎｅｐ阻害剤合成のための新規な方法および中間体
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
JP7138106B2 (ja) 2016-12-23 2022-09-15 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
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 (4)

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EP0212617A1 (en) * 1985-08-23 1987-03-04 Lederle (Japan) Ltd. Process for producing 4-biphenylylacetic acid
WO1998047876A1 (en) * 1997-04-24 1998-10-29 Akzo Nobel N.V. Heterocyclic derivatives and their use as antithrombotic agents
WO2004002977A1 (en) * 2002-07-01 2004-01-08 Pharmacia & Upjohn Company Llc Inhibitors of hcv ns5b polymerase
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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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
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
CN101555211B (zh) * 2009-05-13 2012-01-25 浙江九洲药业股份有限公司 2-酰基氨基-3-联苯基丙酸的化学合成方法

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Publication number Priority date Publication date Assignee Title
EP0212617A1 (en) * 1985-08-23 1987-03-04 Lederle (Japan) Ltd. Process for producing 4-biphenylylacetic acid
WO1998047876A1 (en) * 1997-04-24 1998-10-29 Akzo Nobel N.V. Heterocyclic derivatives and their use as antithrombotic agents
WO2004002977A1 (en) * 2002-07-01 2004-01-08 Pharmacia & Upjohn Company Llc Inhibitors of hcv ns5b polymerase
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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Dicarboxylic Acid Dipeptide Neutral Endopeptidase Inhibitors;Gary M.Ksander,et al.;《J.Med.Chem.》;19950501;第38卷(第10期);1689-1700 *
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Also Published As

Publication number Publication date
CA2772681A1 (en) 2011-03-31
JP5894531B2 (ja) 2016-03-30
RU2012116208A (ru) 2013-11-10
KR20120093227A (ko) 2012-08-22
IN2012DN01968A (enExample) 2015-08-21
JP2013505273A (ja) 2013-02-14
EP2480523A4 (en) 2013-06-26
BR112012006406A2 (pt) 2016-04-12
EP2480523B1 (en) 2017-03-01
EP2480523A1 (en) 2012-08-01
WO2011035569A1 (en) 2011-03-31
KR101821090B1 (ko) 2018-01-22
CA2772681C (en) 2017-01-03
US20160115118A1 (en) 2016-04-28
AU2010297892A1 (en) 2012-03-22
RU2534619C2 (ru) 2014-11-27
CN102639486A (zh) 2012-08-15
AU2010297892B2 (en) 2014-02-06
KR20170002681A (ko) 2017-01-06

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Address after: Jiaojiang District of Taizhou City, Zhejiang province 325000 road outside No. 99

Applicant after: ZHEJIANG JIUZHOU PHARMACEUTICAL Co.,Ltd.

Applicant after: NOVARTIS AG

Address before: Jiaojiang District of Taizhou City, Zhejiang province 325000 road outside No. 99

Applicant before: ZHEJIANG JIUZHOU PHARMACEUTICAL Co.,Ltd.

Applicant before: Novartis AG

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Effective date of registration: 20221018

Address after: No. 18, Tonglian Road, Bixi Street, Changshu, Suzhou, Jiangsu

Patentee after: Ruibo (Suzhou) Pharmaceutical Co.,Ltd.

Patentee after: NOVARTIS AG

Address before: Jiaojiang District of Taizhou City, Zhejiang province 318000 road outside No. 99

Patentee before: ZHEJIANG JIUZHOU PHARMACEUTICAL Co.,Ltd.

Patentee before: NOVARTIS AG