JP6665193B2 - Nep阻害剤を調製するための方法および中間体 - Google Patents

Nep阻害剤を調製するための方法および中間体 Download PDF

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JP6665193B2
JP6665193B2 JP2017542062A JP2017542062A JP6665193B2 JP 6665193 B2 JP6665193 B2 JP 6665193B2 JP 2017542062 A JP2017542062 A JP 2017542062A JP 2017542062 A JP2017542062 A JP 2017542062A JP 6665193 B2 JP6665193 B2 JP 6665193B2
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JP2018506541A (ja
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マーティン,ベンジャミン
マンドレリ,フランセスカ
ヴェントゥロニ,フランセスコ
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ノバルティス アーゲー
ノバルティス アーゲー
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00—Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06—Preparation of nitro compounds
    • C07C201/10—Preparation of nitro compounds by substitution of functional groups by nitro groups
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
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    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0234—Nitrogen-, phosphorus-, arsenic- or antimony-containing compounds
    • B01J31/0235—Nitrogen containing compounds
    • B01J31/0237—Amines
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
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    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0234—Nitrogen-, phosphorus-, arsenic- or antimony-containing compounds
    • B01J31/0235—Nitrogen containing compounds
    • B01J31/0241—Imines or enamines
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
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    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/0234—Nitrogen-, phosphorus-, arsenic- or antimony-containing compounds
    • B01J31/0235—Nitrogen containing compounds
    • B01J31/0244—Nitrogen containing compounds with nitrogen contained as ring member in aromatic compounds or moieties, e.g. pyridine
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    • B01J31/0235—Nitrogen containing compounds
    • B01J31/0245—Nitrogen containing compounds being derivatives of carboxylic or carbonic acids
    • B01J31/0249—Ureas (R2N-C(=O)-NR2)
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    • B01J31/0245—Nitrogen containing compounds being derivatives of carboxylic or carbonic acids
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    • B01J31/0234—Nitrogen-, phosphorus-, arsenic- or antimony-containing compounds
    • B01J31/0255—Phosphorus containing compounds
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    • B01J31/0267—Phosphines or phosphonium compounds, i.e. phosphorus bonded to at least one carbon atom, including e.g. sp2-hybridised phosphorus compounds such as phosphabenzene, the other atoms bonded to phosphorus being either carbon or hydrogen
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    • C07C201/00—Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06—Preparation of nitro compounds
    • C07C201/12—Preparation of nitro compounds by reactions not involving the formation of nitro groups
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    • C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
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    • C07C205/03—Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
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    • C07C205/50—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C205/51—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being saturated
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    • C07C205/53—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
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    • C07C231/00—Preparation of carboxylic acid amides
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • 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
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    • C07C335/04—Derivatives of thiourea
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/535—Organo-phosphoranes
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2017542062A 2015-02-13 2016-02-11 Nep阻害剤を調製するための方法および中間体 Active JP6665193B2 (ja)

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EP15155147 2015-02-13
EP15155147.0 2015-02-13
PCT/IB2016/050725 WO2016128924A1 (en) 2015-02-13 2016-02-11 Process and intermediates for the preparation of nep inhibitors

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JP2018506541A5 JP2018506541A5 (enExample) 2019-08-29
JP6665193B2 true JP6665193B2 (ja) 2020-03-13

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US (1) US10385004B2 (enExample)
EP (1) EP3256444B1 (enExample)
JP (1) JP6665193B2 (enExample)
CN (1) CN107250100B (enExample)
TW (1) TW201632493A (enExample)
WO (1) WO2016128924A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10851059B2 (en) * 2016-08-17 2020-12-01 Novartis Ag Processes and intermediates for NEP inhibitor synthesis
WO2018107158A1 (en) * 2016-12-09 2018-06-14 Celtaxsys, Inc. Monamine and monoamine derivatives as inhibitors of leukotriene a4 hydrolase
CN109053800B (zh) * 2018-07-30 2020-08-14 湖北大学 季鏻盐支载手性氨基-硫脲及其制备方法和用途
CN113121342B (zh) * 2019-12-31 2022-05-31 浙江医药股份有限公司新昌制药厂 一种沙库必曲中间体的制备方法及应用
CN114957043B (zh) * 2022-04-29 2023-09-08 凯特立斯(深圳)科技有限公司 沙库必曲中间体、其制备方法及其应用
CN117902945A (zh) * 2023-12-22 2024-04-19 香港科技大学深圳研究院 手性α-氯代羰基化合物的制备方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5439029A (en) * 1977-09-01 1979-03-24 Sagami Chem Res Center Nitro compounds
US5217996A (en) 1992-01-22 1993-06-08 Ciba-Geigy Corporation Biaryl substituted 4-amino-butyric acid amides
EP1903027A1 (en) * 2006-09-13 2008-03-26 Novartis AG Process for preparing biaryl substituted 4-amino-butyric acid or derivatives thereof and their use in the production of NEP inhibitors
ES2602566T3 (es) 2007-01-12 2017-02-21 Novartis Ag Proceso para preparar ácido 5-bifenil-4-amino-2-metil pentanoico
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
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
PL2435409T3 (pl) * 2009-05-28 2015-01-30 Novartis Ag Podstawione pochodne aminopropionowe jako inhibitory neprylizyny
BR112012006406A2 (pt) 2009-09-23 2016-04-12 Novartis Ag "processo para a fabrição de n-acilbifenil alanina"
ES2550485T3 (es) 2010-01-22 2015-11-10 Novartis Ag Intermedios de inhibidores de la endopeptidasa neutra y método de preparación de los mismos
PT2609075E (pt) 2010-08-23 2016-06-03 Novartis Ag Processo para a preparação de intermediários para o fabrico de inibidores da nep
US9085529B2 (en) 2010-08-23 2015-07-21 Novartis Ag Process for the preparation of intermediates useful for the manufacture NEP inhibitors
AR092278A1 (es) 2012-08-31 2015-04-08 Novartis Ag Proceso de obtencion de derivados n-acilicos de bifenil-alanina e intermediarios relacionados
GB201219300D0 (en) * 2012-10-26 2012-12-12 Isis Innovation Bifunctional organic catalysts
WO2015189862A1 (en) * 2014-06-10 2015-12-17 Council Of Scientific & Industrial Research Chiral amines, a process for preparation and use thereof

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JP2018506541A (ja) 2018-03-08
EP3256444A1 (en) 2017-12-20
WO2016128924A1 (en) 2016-08-18
CN107250100A (zh) 2017-10-13
CN107250100B (zh) 2019-12-06
EP3256444B1 (en) 2019-03-27
TW201632493A (zh) 2016-09-16
US20180022690A1 (en) 2018-01-25
US10385004B2 (en) 2019-08-20

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