PE20091364A1 - Proceso para la preparacion de inhibidores de nep - Google Patents

Proceso para la preparacion de inhibidores de nep

Info

Publication number
PE20091364A1
PE20091364A1 PE2009000047A PE2009000047A PE20091364A1 PE 20091364 A1 PE20091364 A1 PE 20091364A1 PE 2009000047 A PE2009000047 A PE 2009000047A PE 2009000047 A PE2009000047 A PE 2009000047A PE 20091364 A1 PE20091364 A1 PE 20091364A1
Authority
PE
Peru
Prior art keywords
formula
compound
preparation
alkaline
ammonium
Prior art date
Application number
PE2009000047A
Other languages
English (en)
Inventor
David Hook
Daniel Kaufmann
Erhard Bappert
Philippe Polleux
Bernhard Riss
Matthias Napp
Jonathan Medlock
Antonio Zanotti-Gerosa
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20091364A1 publication Critical patent/PE20091364A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—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 two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/38—2-Pyrrolones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/18—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—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 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—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 two double bonds between ring members or between ring members and non-ring members 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
    • C07D207/36—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/22—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from lactams, cyclic ketones or cyclic oximes, e.g. by reactions involving Beckmann rearrangement
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

SE REFIERE A UN PROCESO PARA LA PREPARACION DE UN COMPUESTO DE FORMULA (7) DONDE R1 ES H O UN GRUPO PROTECTOR DE N; R6 Y R7 SON CADA UNO ALQUILO, ARILO, ARIL-ALQUILO, CICLOALQUILO, ENTRE OTROS; EN DONDE DICHO PROCESO COMPRENDE: A) HACER REACCIONAR UN COMPUESTO DE FORMULA (8) i) CON UNA AMINA DE FORMULA (13), (14) O (15) Y OPCIONALMENTE UNA SAL DE METAL ALCALINO, DE AMONIO, ENTRE OTROS; ii) CON UN COMPUESTO PREPARADO CON LA MEZCLA DE UN COMPUESTO DE FORMULA (18) CON UN ALCOHOLATO DE FORMULA M-O-R8 Y OPCIONALMENTE TRATADO CON UNA SAL M1X'; O iii) CON MEZCLAS DE LOS MISMOS; EN DONDE R8 ES CARBOXILATO O TRIBROMURO; X Y X' SON CADA UNO UN ANION TAL COMO HALURO, PERCLORATO, ENTRE OTROS; M ES UN METAL ALCALINO O ALCALINOTERREO; M1 ES UN METAL ALCALINO, AMONIO, ENTRE OTROS. DICHOS COMPUESTOS SON INTERMEDIARIOS PARA LA PREPARACION DE UN COMPUESTO DE FORMULA (1) DONDE R3 ES CARBOXILO O ESTER, QUE INHIBEN LA ENDOPEPTIDASA NEUTRA (NEP)
PE2009000047A 2008-01-17 2009-01-15 Proceso para la preparacion de inhibidores de nep PE20091364A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08150353 2008-01-17

Publications (1)

Publication Number Publication Date
PE20091364A1 true PE20091364A1 (es) 2009-10-13

Family

ID=40758693

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000047A PE20091364A1 (es) 2008-01-17 2009-01-15 Proceso para la preparacion de inhibidores de nep

Country Status (29)

Country Link
US (4) US8580974B2 (es)
EP (1) EP2245009B1 (es)
JP (2) JP5739667B2 (es)
KR (1) KR101587668B1 (es)
CN (2) CN101952249B (es)
AR (1) AR070176A1 (es)
AU (1) AU2009204759B2 (es)
BR (1) BRPI0906764A2 (es)
CA (1) CA2711529C (es)
CL (1) CL2009000089A1 (es)
CO (1) CO6290677A2 (es)
EC (1) ECSP10010405A (es)
ES (1) ES2602564T3 (es)
GT (1) GT201000211A (es)
HU (1) HUE030606T2 (es)
IL (1) IL206664A0 (es)
MA (1) MA31951B1 (es)
MX (1) MX2010007842A (es)
MY (1) MY169425A (es)
NZ (2) NZ600119A (es)
PE (1) PE20091364A1 (es)
PL (1) PL2245009T3 (es)
PT (1) PT2245009T (es)
RU (2) RU2513521C2 (es)
SG (1) SG187491A1 (es)
SI (1) SI2245009T1 (es)
TN (1) TN2010000304A1 (es)
TW (1) TWI422370B (es)
WO (1) WO2009090251A2 (es)

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JP6301371B2 (ja) 2013-02-14 2018-04-11 ノバルティス アーゲー インビボ効力が改善されたｎｅｐ阻害剤としての置換ビスフェニルブタン酸誘導体
US8901169B2 (en) 2013-03-05 2014-12-02 Theravance Biopharma R&D Ip, Llc Neprilysin inhibitors
ES2957314T3 (es) * 2013-11-15 2024-01-17 Hoffmann La Roche Procesos para la preparación de compuestos de pirimidinilciclopentano
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WO2015116760A1 (en) 2014-01-30 2015-08-06 Theravance Biopharma R&D Ip, Llc 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
HUE046278T2 (hu) 2014-11-14 2020-02-28 Zentiva Ks Módszer AHU-377 gyógyszerészetben alkalmazható formáinak elõállítására, izolálására és tisztítására
ES2727384T3 (es) * 2014-12-19 2019-10-15 Basf Se Procedimiento para la preparación de compuestos carbonílicos ópticamente activos
CN107257785B (zh) 2015-02-11 2020-07-07 施万生物制药研发Ip有限责任公司 作为脑啡肽酶抑制剂的(2s,4r)-5-(5’-氯-2’-氟联苯-4-基)-4-(乙氧基草酰基氨基)-2-羟甲基-2-甲基戊酸
TW201632493A (zh) 2015-02-13 2016-09-16 諾華公司 新穎方法
SI3259255T1 (sl) 2015-02-19 2021-04-30 Theravance Biopharma R&D Ip, Llc (2R,4R)-5-(5'-kloro-2'-fluorobifenil-4-IL)-2-hidroksi-4-((5-metiloksa- zol-2-karbonil)amino)pentanojska kislina
CN106146351B (zh) * 2015-04-03 2020-09-11 博瑞生物医药（苏州）股份有限公司 制备联芳基取代的4-氨基-丁酸或其衍生物的方法
CN105061263B (zh) * 2015-08-11 2017-03-15 苏州楚凯药业有限公司 一种nep抑制剂中间体的制备方法
CN105152980B (zh) * 2015-09-11 2017-03-29 浙江永宁药业股份有限公司 N‑叔丁氧羰基‑（4s）‑（对苯基苯基甲基）‑4‑氨基‑（2r）‑甲基丁酸的手性制备方法
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JO3771B1 (ar) 2015-12-10 2021-01-31 Novartis Ag متوسطات لتحضير ساكوبيتريل وتحضيرها
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KR20220035991A (ko) 2016-03-08 2022-03-22 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 (2s,4r)-5-(5'-클로로-2'-플루오로-[1,1'-비페닐]-4-일)-2-(에톡시메틸)-4-(3-히드록시이속사졸-5-카르복사미도)-2-메틸펜탄산 결정 및 그 용도
CN109415308B (zh) 2016-07-05 2022-09-06 诺华股份有限公司 用于早期沙卡布曲中间体的新方法
CN109563019A (zh) 2016-08-17 2019-04-02 诺华股份有限公司 Nep抑制剂合成的新方法和中间体
EP3558930B1 (en) 2016-12-23 2021-05-26 Novartis AG New process for early sacubitril intermediates
EP3421455B1 (en) * 2017-06-29 2019-03-27 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Improved process for the preparation of chiral 3-amino-piperidins, useful intermediates for the preparation of tofacitinib
CN109912508B (zh) * 2019-04-30 2022-08-12 上海天慈国际药业有限公司 一种右美托咪定及其盐酸盐的制备方法
CN110878039A (zh) * 2019-12-18 2020-03-13 株洲千金药业股份有限公司 一种沙库巴曲缬沙坦钠杂质的制备方法
CN115611857B (zh) * 2022-09-09 2024-05-31 上海伍夫科技有限公司 一种2-甲基-5-（1-甲基吡咯烷-2-基）吡啶的制备方法
CN115772088A (zh) * 2022-12-28 2023-03-10 海门瑞一医药科技有限公司 一种叔丁氧基（双二甲胺基）甲烷的制备方法
CN118239990A (zh) * 2024-05-28 2024-06-25 北京元延医药科技股份有限公司 不对称氢化催化合成药物的稀有贵金属和手性膦的配合物

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