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AR120456A1 - Síntesis mejorada del compuesto inhibidor de g12c de kras - Google Patents

Síntesis mejorada del compuesto inhibidor de g12c de kras

Info

Publication number
AR120456A1
AR120456A1 ARP200103144A ARP200103144A AR120456A1 AR 120456 A1 AR120456 A1 AR 120456A1 AR P200103144 A ARP200103144 A AR P200103144A AR P200103144 A ARP200103144 A AR P200103144A AR 120456 A1 AR120456 A1 AR 120456A1
Authority
AR
Argentina
Prior art keywords
compound
formula
reacting
kras
preparing
Prior art date
Application number
ARP200103144A
Other languages
English (en)
Inventor
Michael Thomas Corbett
Sebastien Caille
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of AR120456A1 publication Critical patent/AR120456A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente divulgación se refiere a un proceso mejorado, eficaz y escalable para preparar compuestos intermedios tales como 2-isopropil-4-metilpiridin-3-amina, útiles para síntesis de compuestos, tales como el compuesto de fórmula (1), para el tratamiento de cánceres con mutaciones en G12C de KRAS. Reivindicación 1: Un método para preparar un compuesto de fórmula (2), comprendiendo el método hacer reaccionar una mezcla que comprende un compuesto que tiene la estructura de fórmula (3) con paladio en presencia de hidrógeno en un disolvente. Reivindicación 3: Un método para preparar un compuesto de fórmula (2), comprendiendo el método hacer reaccionar una mezcla que comprende una solución acuosa de NaOH, un compuesto que tiene la estructura: de fórmula (4) e hipoclorito de sodio. Reivindicación 7: Un método para preparar un compuesto, que tiene la estructura: de fórmula (5) comprendiendo el método hacer reaccionar una mezcla que comprende las etapas: a.) haciendo reaccionar crotonaldehído y (S)-a,a-bis[3,5-bis(trifluorometil)fenil]-2-pirrolidinametanol trimetilsilil éter; b.) 4-metil-3-oxopentanonitrilo; c.) acetonitrilo; y d.) clorhidrato de hidroxilamina.
ARP200103144A 2019-11-14 2020-11-13 Síntesis mejorada del compuesto inhibidor de g12c de kras AR120456A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201962935515P 2019-11-14 2019-11-14

Publications (1)

Publication Number Publication Date
AR120456A1 true AR120456A1 (es) 2022-02-16

Family

ID=73740592

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200103144A AR120456A1 (es) 2019-11-14 2020-11-13 Síntesis mejorada del compuesto inhibidor de g12c de kras

Country Status (9)

Country Link
US (3) US12473281B2 (es)
EP (1) EP4058432A1 (es)
JP (1) JP2023501522A (es)
AR (1) AR120456A1 (es)
AU (1) AU2020383535A1 (es)
CA (1) CA3161156A1 (es)
MX (1) MX2022005726A (es)
TW (1) TW202132271A (es)
WO (1) WO2021097207A1 (es)

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JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3807276B1 (en) 2018-06-12 2025-12-10 Amgen Inc. Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
AU2020277398B2 (en) 2019-05-21 2026-01-29 Amgen Inc. Solid state forms
JP7092935B2 (ja) 2019-05-21 2022-06-28 アムジエン・インコーポレーテツド 固体形態
WO2021047603A1 (zh) * 2019-09-11 2021-03-18 凯瑞斯德生化(苏州)有限公司 一种应用于kras抑制剂类药物杂环中间体的合成方法
TW202132271A (zh) 2019-11-14 2021-09-01 美商安進公司 Ｋｒａｓ ｇ１２ｃ抑制劑化合物之改善的合成
BR112022009390A2 (pt) 2019-11-14 2022-08-09 Amgen Inc Síntese melhorada de composto inibidor de kras g12c
CN114585624A (zh) * 2020-06-02 2022-06-03 上海喆邺生物科技有限公司 一种手性中间体及其制备方法
EP4247813B1 (en) 2020-11-20 2025-12-24 Amgen, Inc Process for preparing 7-chloro-6-fluoro-1-(2-isopropyl-4-methylpyridin-3- yl)pyridof[2,3-d]pyrimidine-2,4(1h,3h)-dione
CN113666865B (zh) * 2021-09-07 2023-05-26 杭州科耀医药科技有限公司 一种2-异丙基-3-氨基-4-甲基吡啶的合成方法
EP4426303B1 (en) 2021-11-02 2025-10-08 Semmelweis Egyetem Farnesyl-transferase inhibitors and kras inhibitors for treating kras mutant cancers
AU2023230882A1 (en) 2022-03-07 2024-08-22 Amgen Inc. A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile.
CN114907259A (zh) * 2022-04-28 2022-08-16 常州中氪生命科学技术有限公司 一种索托拉西布中间体的合成方法
CN115466259B (zh) * 2022-08-16 2023-12-05 山东大学 一种kras g12c抑制剂索托拉西布的制备方法

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