KR102128127B1 - 5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법 - Google Patents

5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법 Download PDF

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KR102128127B1
KR102128127B1 KR1020157010087A KR20157010087A KR102128127B1 KR 102128127 B1 KR102128127 B1 KR 102128127B1 KR 1020157010087 A KR1020157010087 A KR 1020157010087A KR 20157010087 A KR20157010087 A KR 20157010087A KR 102128127 B1 KR102128127 B1 KR 102128127B1
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pyridin
trifluoromethyl
amine
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acetamide
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KR20150072408A (ko
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디트마르 플루바허
니콜 비에리
무라트 아체모글루
파스칼 미셀
라스무스 모스
한스 스테틀러
마리아 카테리나 테스타
외르크 브로지오
프랑크 새퍼
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노파르티스 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
KR1020157010087A 2012-10-23 2013-10-21 5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법 Active KR102128127B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261717237P 2012-10-23 2012-10-23
US61/717,237 2012-10-23
US201361842101P 2013-07-02 2013-07-02
US61/842,101 2013-07-02
PCT/EP2013/071996 WO2014064058A1 (en) 2012-10-23 2013-10-21 Improved process for manufacturing 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine

Publications (2)

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KR20150072408A KR20150072408A (ko) 2015-06-29
KR102128127B1 true KR102128127B1 (ko) 2020-06-30

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US (1) US9637468B2 (enExample)
EP (1) EP2912030B1 (enExample)
JP (1) JP6267213B2 (enExample)
KR (1) KR102128127B1 (enExample)
CN (1) CN104736532B (enExample)
AU (2) AU2013336807B2 (enExample)
BR (1) BR112015007243B1 (enExample)
CA (1) CA2885471C (enExample)
ES (1) ES2605638T3 (enExample)
IN (1) IN2015DN01331A (enExample)
MX (1) MX360703B (enExample)
PL (1) PL2912030T3 (enExample)
PT (1) PT2912030T (enExample)
RU (1) RU2646760C2 (enExample)
WO (1) WO2014064058A1 (enExample)

Families Citing this family (12)

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JP6026544B2 (ja) 2011-09-27 2016-11-16 ノバルティス アーゲー 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
WO2014110466A1 (en) * 2013-01-12 2014-07-17 Dawei Zhang Pyridine compounds used as pi3 kinase inhibitors
HK1213251A1 (zh) 2013-03-14 2016-06-30 Novartis Ag 作为突变idh抑制剂的3-嘧啶-4-基-恶唑烷-2-酮化合物
BR112016023811B8 (pt) 2014-04-22 2023-01-10 Piqur Therapeutics Ag Método para fabricação para derivados de triazina, pirimidina e piridina, seus intermediários e seus métodos de fabricação
CN107001317B (zh) * 2014-09-29 2019-05-24 山东轩竹医药科技有限公司 高选择性取代嘧啶类pi3k抑制剂
CN105085476B (zh) * 2014-11-24 2018-03-09 苏州晶云药物科技有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法
CN105001151B (zh) * 2015-08-28 2017-07-14 苏州明锐医药科技有限公司 布帕尼西中间体及其制备方法
CN106543140A (zh) * 2015-09-21 2017-03-29 苏州晶云药物科技有限公司 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法
CN107793394A (zh) * 2017-08-03 2018-03-13 上海厚璞生物科技有限公司 一种生产选择性pi3k抑制剂的系列关键中间体
BR112021011330A2 (pt) * 2018-12-18 2021-08-31 Astrazeneca Ab Processo farmacêutico e intermediários

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012044727A2 (en) * 2010-10-01 2012-04-05 Novartis Ag Manufacturing process for pyrimidine derivatives

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WO2002062805A1 (en) * 2001-02-08 2002-08-15 Toyama Chemical Co., Ltd. 6-substituted alkylamino-3-pyridylboric acid derivative or salt thereof and processes for producing these
PT2316831E (pt) * 2002-11-21 2013-06-06 Novartis Ag 2-(morfolin-4-il)pirimidinas como inibidores da fosfatidilinositol (pi) quinase e a sua utilização no tratamento do cancro
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012044727A2 (en) * 2010-10-01 2012-04-05 Novartis Ag Manufacturing process for pyrimidine derivatives

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CA2885471A1 (en) 2014-05-01
CN104736532A (zh) 2015-06-24
AU2013336807B2 (en) 2016-10-27
EP2912030A1 (en) 2015-09-02
AU2013336807A1 (en) 2015-03-05
US20150246897A1 (en) 2015-09-03
ES2605638T3 (es) 2017-03-15
JP2016502510A (ja) 2016-01-28
BR112015007243B1 (pt) 2022-02-08
JP6267213B2 (ja) 2018-01-24
AU2016238941A1 (en) 2016-11-03
CA2885471C (en) 2021-02-23
IN2015DN01331A (enExample) 2015-07-03
BR112015007243A2 (pt) 2017-07-04
CN104736532B (zh) 2017-04-05
RU2015119259A (ru) 2016-12-20
MX360703B (es) 2018-11-14
US9637468B2 (en) 2017-05-02
RU2646760C2 (ru) 2018-03-07
PL2912030T3 (pl) 2017-02-28
WO2014064058A1 (en) 2014-05-01
KR20150072408A (ko) 2015-06-29
PT2912030T (pt) 2016-11-30
EP2912030B1 (en) 2016-08-31
MX2015005188A (es) 2015-09-07

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