CN104736532B - 改进的生产5‑(2,6‑二‑4‑吗啉‑4‑嘧啶)‑4‑三氟甲基吡啶‑2‑胺的方法 - Google Patents
改进的生产5‑(2,6‑二‑4‑吗啉‑4‑嘧啶)‑4‑三氟甲基吡啶‑2‑胺的方法 Download PDFInfo
- Publication number
- CN104736532B CN104736532B CN201380055482.4A CN201380055482A CN104736532B CN 104736532 B CN104736532 B CN 104736532B CN 201380055482 A CN201380055482 A CN 201380055482A CN 104736532 B CN104736532 B CN 104736532B
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- China
- Prior art keywords
- trifluoromethyl
- acetamide
- amine
- bases
- pyridine
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- Legal status (The legal status 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 status listed.)
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- CWHUFRVAEUJCEF-UHFFFAOYSA-N Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(N2CCOCC2)c1 Chemical compound Nc(nc1)cc(C(F)(F)F)c1-c1nc(N2CCOCC2)nc(N2CCOCC2)c1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- 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
Landscapes
- 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)
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)
| Publication Number | Publication Date |
|---|---|
| CN104736532A CN104736532A (zh) | 2015-06-24 |
| CN104736532B true CN104736532B (zh) | 2017-04-05 |
Family
ID=49448162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380055482.4A Active CN104736532B (zh) | 2012-10-23 | 2013-10-21 | 改进的生产5‑(2,6‑二‑4‑吗啉‑4‑嘧啶)‑4‑三氟甲基吡啶‑2‑胺的方法 |
Country Status (15)
| Country | Link |
|---|---|
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI547493B (zh) | 2011-09-27 | 2016-09-01 | 諾華公司 | 作為突變ｉｄｈ之抑制劑之３－嘧啶－４－基－唑啶－２－酮 |
| 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 |
| CN105050602B (zh) * | 2013-01-12 | 2018-05-25 | 张大为 | 作为pi3激酶抑制剂的吡啶化合物 |
| WO2014141104A1 (en) | 2013-03-14 | 2014-09-18 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| JP6513105B2 (ja) | 2014-04-22 | 2019-05-15 | ウニヴェルズィテート バーゼル | トリアジン、ピリミジン及びピリジン誘導体の新規製造方法 |
| WO2016050201A1 (zh) * | 2014-09-29 | 2016-04-07 | 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012044727A2 (en) * | 2010-10-01 | 2012-04-05 | Novartis Ag | Manufacturing process for pyrimidine derivatives |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MXPA05005477A (es) * | 2002-11-21 | 2005-07-25 | Chiron Corp | Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer. |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
-
2013
- 2013-10-21 PT PT137798419T patent/PT2912030T/pt unknown
- 2013-10-21 IN IN1331DEN2015 patent/IN2015DN01331A/en unknown
- 2013-10-21 US US14/437,177 patent/US9637468B2/en active Active
- 2013-10-21 ES ES13779841.9T patent/ES2605638T3/es active Active
- 2013-10-21 RU RU2015119259A patent/RU2646760C2/ru active
- 2013-10-21 KR KR1020157010087A patent/KR102128127B1/ko active Active
- 2013-10-21 CA CA2885471A patent/CA2885471C/en active Active
- 2013-10-21 MX MX2015005188A patent/MX360703B/es active IP Right Grant
- 2013-10-21 WO PCT/EP2013/071996 patent/WO2014064058A1/en not_active Ceased
- 2013-10-21 CN CN201380055482.4A patent/CN104736532B/zh active Active
- 2013-10-21 BR BR112015007243-7A patent/BR112015007243B1/pt active IP Right Grant
- 2013-10-21 JP JP2015538398A patent/JP6267213B2/ja active Active
- 2013-10-21 AU AU2013336807A patent/AU2013336807B2/en active Active
- 2013-10-21 EP EP13779841.9A patent/EP2912030B1/en active Active
- 2013-10-21 PL PL13779841T patent/PL2912030T3/pl unknown
-
2016
- 2016-10-07 AU AU2016238941A patent/AU2016238941A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012044727A2 (en) * | 2010-10-01 | 2012-04-05 | Novartis Ag | Manufacturing process for pyrimidine derivatives |
Non-Patent Citations (1)
| Title |
|---|
| Preparation and Diels-Alder/cross coupling reactions of a 2-diethanolaminoboron-substituted 1,3-dienes;Liqiong Wang et al.;《Beilstein Journal of Organic Chemistry》;20090921;第5卷(第45期);第39篇 * |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2015005188A (es) | 2015-09-07 |
| CA2885471C (en) | 2021-02-23 |
| CA2885471A1 (en) | 2014-05-01 |
| US9637468B2 (en) | 2017-05-02 |
| IN2015DN01331A (enExample) | 2015-07-03 |
| RU2015119259A (ru) | 2016-12-20 |
| RU2646760C2 (ru) | 2018-03-07 |
| BR112015007243B1 (pt) | 2022-02-08 |
| JP2016502510A (ja) | 2016-01-28 |
| KR20150072408A (ko) | 2015-06-29 |
| US20150246897A1 (en) | 2015-09-03 |
| WO2014064058A1 (en) | 2014-05-01 |
| EP2912030A1 (en) | 2015-09-02 |
| MX360703B (es) | 2018-11-14 |
| PT2912030T (pt) | 2016-11-30 |
| AU2013336807A1 (en) | 2015-03-05 |
| PL2912030T3 (pl) | 2017-02-28 |
| AU2016238941A1 (en) | 2016-11-03 |
| AU2013336807B2 (en) | 2016-10-27 |
| ES2605638T3 (es) | 2017-03-15 |
| CN104736532A (zh) | 2015-06-24 |
| EP2912030B1 (en) | 2016-08-31 |
| JP6267213B2 (ja) | 2018-01-24 |
| KR102128127B1 (ko) | 2020-06-30 |
| BR112015007243A2 (pt) | 2017-07-04 |
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Legal Events
| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| EXSB | Decision made by sipo to initiate substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| EE01 | Entry into force of recordation of patent licensing contract |
Application publication date: 20150624 Assignee: Hangzhou Arnold Biomedical Technology Co.,Ltd. Assignor: NOVARTIS AG Contract record no.: X2021990000669 Denomination of invention: Improved method for producing 5 - (2,6-di-4-morpholine-4-pyrimidine) - 4-trifluoromethylpyridine-2-amine Granted publication date: 20170405 License type: Exclusive License Record date: 20211102 |
|
| EE01 | Entry into force of recordation of patent licensing contract |