PE20231013A1 - Procesos e intermedios para la preparacion de (s)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1h-pirazol-4-carboxamida - Google Patents

Procesos e intermedios para la preparacion de (s)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1h-pirazol-4-carboxamida

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Publication number
PE20231013A1
PE20231013A1 PE2023001132A PE2023001132A PE20231013A1 PE 20231013 A1 PE20231013 A1 PE 20231013A1 PE 2023001132 A PE2023001132 A PE 2023001132A PE 2023001132 A PE2023001132 A PE 2023001132A PE 20231013 A1 PE20231013 A1 PE 20231013A1
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PE
Peru
Prior art keywords
methyl
fluoro
phenyl
amino
methoxybenzamido
Prior art date
Application number
PE2023001132A
Other languages
English (en)
Inventor
Delgado Alonso Jose Arguelles
Charles Todd Eary
Jared Wade Fennell
Scott Alan Frank
Nicholas Andrew Magnus
Elizabeth Ann Mcfaddin
Roger Ryan Rothhaar
Stacey Renee Spencer
Radhe Krishan Vaid
Original Assignee
Loxo Oncology Inc
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 Loxo Oncology Inc filed Critical Loxo Oncology Inc
Publication of PE20231013A1 publication Critical patent/PE20231013A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/01Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/30Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same unsaturated acyclic carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/01Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/42Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms
    • C07C255/44Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being further bound to other hetero atoms at least one of the singly-bound nitrogen atoms being acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/022Boron compounds without C-boron linkages
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic 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 (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1H-pirazol-4-carboxamid, que comprende las etapas de (viii) acoplar el compuesto de Formula (III) y [(1S)-2,2,2-trifluoro-1-metil-etil]hidrazina para dar N-[[4-[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metil-etil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida y (ix) sintetizar (S)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1Hpirazol-4-carboxamida a partir de N-[[4-[5-amino-4-ciano-1-[(1S)-2,2,2-trifluoro-1-metil-etil]pirazol-3-il]fenil]metil]-5-fluoro-2-metoxi-benzamida.
PE2023001132A 2020-09-10 2021-09-09 Procesos e intermedios para la preparacion de (s)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1h-pirazol-4-carboxamida PE20231013A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063076577P 2020-09-10 2020-09-10
PCT/US2021/049621 WO2022056100A1 (en) 2020-09-10 2021-09-09 Processes and intermediates for the preparation of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropane-2-yl)-1h-pyrazole-4-carboxamide

Publications (1)

Publication Number Publication Date
PE20231013A1 true PE20231013A1 (es) 2023-07-05

Family

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PE2023001132A PE20231013A1 (es) 2020-09-10 2021-09-09 Procesos e intermedios para la preparacion de (s)-5-amino-3-(4-((5-fluoro-2-metoxibenzamido)metil)fenil)-1-(1,1,1-trifluoropropan-2-il)-1h-pirazol-4-carboxamida

Country Status (17)

Country Link
US (1) US20230322682A1 (es)
EP (1) EP4211117A1 (es)
JP (1) JP2023540802A (es)
KR (1) KR20230065307A (es)
CN (1) CN116323553A (es)
AR (1) AR123427A1 (es)
AU (2) AU2021342132B2 (es)
BR (1) BR112023002873A2 (es)
CA (1) CA3189884A1 (es)
CL (1) CL2023000666A1 (es)
CO (1) CO2023002865A2 (es)
EC (1) ECSP23017104A (es)
IL (1) IL301103A (es)
MX (1) MX2023002890A (es)
PE (1) PE20231013A1 (es)
TW (2) TW202317099A (es)
WO (1) WO2022056100A1 (es)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MD20150035A2 (ro) * 2012-11-02 2015-10-31 Pfizer Inc. Inhibitori de tirozinkinaza Bruton
UA127863C2 (uk) * 2015-12-16 2024-01-31 Локсо Онколоджі, Інк. Сполуки, які можна застосовувати як інгібітори кінази
CN107382973B (zh) * 2016-05-16 2020-08-07 苏州信诺维医药科技有限公司 作为btk抑制剂的5-氨基吡唑甲酰胺衍生物及其制备方法和药物组合物
CN107652294A (zh) * 2017-11-14 2018-02-02 安徽诺全药业有限公司 一种伊鲁替尼的制备方法
US20210330643A1 (en) 2018-07-31 2021-10-28 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide

Also Published As

Publication number Publication date
AU2024202587A1 (en) 2024-05-09
CN116323553A (zh) 2023-06-23
AU2021342132B2 (en) 2024-05-23
IL301103A (en) 2023-05-01
TW202225146A (zh) 2022-07-01
AR123427A1 (es) 2022-11-30
EP4211117A1 (en) 2023-07-19
US20230322682A1 (en) 2023-10-12
TW202317099A (zh) 2023-05-01
BR112023002873A2 (pt) 2023-03-21
AU2021342132A1 (en) 2023-04-13
CO2023002865A2 (es) 2023-03-27
WO2022056100A1 (en) 2022-03-17
ECSP23017104A (es) 2023-04-28
CA3189884A1 (en) 2022-03-17
KR20230065307A (ko) 2023-05-11
MX2023002890A (es) 2023-04-04
TWI809489B (zh) 2023-07-21
CL2023000666A1 (es) 2023-08-18
JP2023540802A (ja) 2023-09-26

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