JP2014532058A - ５−［２−［７−（トリフルオロメチル）−５−［４−（トリフルオロメチル）フェニル］ピラゾロ［１，５−ａ］ピリミジン−３−イル］エチニル］−２−ピリジンアミンの製造方法 - Google Patents
５−［２−［７−（トリフルオロメチル）−５−［４−（トリフルオロメチル）フェニル］ピラゾロ［１，５−ａ］ピリミジン−３−イル］エチニル］−２−ピリジンアミンの製造方法 Download PDFInfo
- Publication number
- JP2014532058A JP2014532058A JP2014533842A JP2014533842A JP2014532058A JP 2014532058 A JP2014532058 A JP 2014532058A JP 2014533842 A JP2014533842 A JP 2014533842A JP 2014533842 A JP2014533842 A JP 2014533842A JP 2014532058 A JP2014532058 A JP 2014532058A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- providing
- inert solvent
- producing
- reacting
- Prior art date
- 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.)
- Pending
Links
- 0 C*C(CC(c1ccc(**)cc1)=O)=O Chemical compound C*C(CC(c1ccc(**)cc1)=O)=O 0.000 description 6
Classifications
-
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
-
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/0825—Preparations of compounds not comprising Si-Si or Si-cyano linkages
- C07F7/083—Syntheses without formation of a Si-C 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
- C07D213/73—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161542837P | 2011-10-04 | 2011-10-04 | |
| US61/542,837 | 2011-10-04 | ||
| US201261684181P | 2012-08-17 | 2012-08-17 | |
| US61/684,181 | 2012-08-17 | ||
| PCT/EP2012/069303 WO2013050310A1 (en) | 2011-10-04 | 2012-10-01 | Methods for the preparation of 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014532058A true JP2014532058A (ja) | 2014-12-04 |
| JP2014532058A5 JP2014532058A5 (enExample) | 2015-11-19 |
Family
ID=46963723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014533842A Pending JP2014532058A (ja) | 2011-10-04 | 2012-10-01 | ５−［２−［７−（トリフルオロメチル）−５−［４−（トリフルオロメチル）フェニル］ピラゾロ［１，５−ａ］ピリミジン−３−イル］エチニル］−２−ピリジンアミンの製造方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US9447099B2 (enExample) |
| EP (1) | EP2763991B1 (enExample) |
| JP (1) | JP2014532058A (enExample) |
| KR (1) | KR20140071474A (enExample) |
| CN (1) | CN103857679A (enExample) |
| AR (1) | AR088098A1 (enExample) |
| AU (1) | AU2012320732A1 (enExample) |
| BR (1) | BR112014007850A2 (enExample) |
| CA (1) | CA2847092A1 (enExample) |
| IL (1) | IL231283A0 (enExample) |
| MX (1) | MX2014004062A (enExample) |
| RU (1) | RU2630700C2 (enExample) |
| SG (2) | SG2014014203A (enExample) |
| WO (1) | WO2013050310A1 (enExample) |
| ZA (1) | ZA201401398B (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2016013711A (es) * | 2014-04-23 | 2017-01-13 | Hoffmann La Roche | Antagonistas de receptores de glumato metabotropicos 2/3 (mglu2/3) para el tratamiento de varias discapacidades intelectuales. |
| CA3085001C (en) * | 2019-05-20 | 2021-10-05 | Mabplex International, Ltd. | One-pot process for preparing intermediate of antibody-drug conjugate |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007528395A (ja) * | 2004-03-09 | 2007-10-11 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 慢性炎症性疾患の治療のためのサイトカイン生成のインヒビターとしての３−‘４−複素環−１，２，３−トリアゾール−１−イル−ｎ−アリール−ベンズアミド |
| JP2008534455A (ja) * | 2005-03-23 | 2008-08-28 | エフ．ホフマン−ラ ロシュ アーゲー | ｍＧｌｕＲ２アンタゴニストとしてのアセチレニル−ピラゾロ−ピリミジン誘導体 |
| WO2010060952A1 (en) * | 2008-11-27 | 2010-06-03 | Boehringer Ingelheim International Gmbh | 6,7,8,9-tetrahydro-5h-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them |
| WO2011014520A2 (en) * | 2009-07-29 | 2011-02-03 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA05013233A (es) | 2003-06-12 | 2006-03-09 | Hoffmann La Roche | Derivados de imidazol heteroaril-substituidos como antagonistas del receptor de glutamato. |
| US7329662B2 (en) * | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| ATE512966T1 (de) * | 2005-02-11 | 2011-07-15 | Hoffmann La Roche | Pyrazolo-pyrimidin-derivate als mglur2- antagonisten |
| ATE463495T1 (de) * | 2005-09-27 | 2010-04-15 | Hoffmann La Roche | Oxadiazolylpyrazolopyrimidine als mglur2- antagonisten |
-
2012
- 2012-09-27 US US13/628,069 patent/US9447099B2/en not_active Expired - Fee Related
- 2012-10-01 EP EP12766655.0A patent/EP2763991B1/en not_active Not-in-force
- 2012-10-01 MX MX2014004062A patent/MX2014004062A/es unknown
- 2012-10-01 RU RU2014116885A patent/RU2630700C2/ru not_active IP Right Cessation
- 2012-10-01 JP JP2014533842A patent/JP2014532058A/ja active Pending
- 2012-10-01 KR KR1020147011727A patent/KR20140071474A/ko not_active Ceased
- 2012-10-01 SG SG2014014203A patent/SG2014014203A/en unknown
- 2012-10-01 WO PCT/EP2012/069303 patent/WO2013050310A1/en not_active Ceased
- 2012-10-01 BR BR112014007850A patent/BR112014007850A2/pt active Search and Examination
- 2012-10-01 CA CA2847092A patent/CA2847092A1/en not_active Abandoned
- 2012-10-01 AU AU2012320732A patent/AU2012320732A1/en not_active Abandoned
- 2012-10-01 SG SG10201507001RA patent/SG10201507001RA/en unknown
- 2012-10-01 CN CN201280048837.2A patent/CN103857679A/zh active Pending
- 2012-10-02 AR ARP120103667A patent/AR088098A1/es unknown
-
2014
- 2014-02-24 ZA ZA2014/01398A patent/ZA201401398B/en unknown
- 2014-03-03 IL IL231283A patent/IL231283A0/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007528395A (ja) * | 2004-03-09 | 2007-10-11 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | 慢性炎症性疾患の治療のためのサイトカイン生成のインヒビターとしての３−‘４−複素環−１，２，３−トリアゾール−１−イル−ｎ−アリール−ベンズアミド |
| JP2008534455A (ja) * | 2005-03-23 | 2008-08-28 | エフ．ホフマン−ラ ロシュ アーゲー | ｍＧｌｕＲ２アンタゴニストとしてのアセチレニル−ピラゾロ−ピリミジン誘導体 |
| WO2010060952A1 (en) * | 2008-11-27 | 2010-06-03 | Boehringer Ingelheim International Gmbh | 6,7,8,9-tetrahydro-5h-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them |
| WO2011014520A2 (en) * | 2009-07-29 | 2011-02-03 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
Non-Patent Citations (3)
| Title |
|---|
| A. ELANGOVAN ET AL: "Sonogashira coupling reaction with diminished homocoupling", ORGANIC LETTERS, vol. 5(11), JPN7016001247, 2003, pages 1841 - 1844, ISSN: 0003319901 * |
| R. CHINCHILLA ET AL: "The Sonogashira Reaction: A Booming Methodology in Synthetic Organic Chemistry", CHEMICAL REVIEWS, vol. 107, JPN7016001249, 2007, pages 874 - 922, ISSN: 0003319903 * |
| YIN, LUNXIANG: "Synthesis of new calcineurin inhibitors via Pd-catalyzed cross-coupling reactions", DISSERTATION OF HUMBOLDT UNIVERSITY OF BERLIN, JPN7016001248, 2005, ISSN: 0003319902 * |
Also Published As
| Publication number | Publication date |
|---|---|
| RU2630700C2 (ru) | 2017-09-12 |
| US20130085278A1 (en) | 2013-04-04 |
| RU2014116885A (ru) | 2015-11-10 |
| ZA201401398B (en) | 2017-04-26 |
| CA2847092A1 (en) | 2013-04-11 |
| AR088098A1 (es) | 2014-05-07 |
| SG2014014203A (en) | 2014-05-29 |
| IL231283A0 (en) | 2014-04-30 |
| WO2013050310A1 (en) | 2013-04-11 |
| EP2763991A1 (en) | 2014-08-13 |
| EP2763991B1 (en) | 2016-12-28 |
| US9447099B2 (en) | 2016-09-20 |
| AU2012320732A1 (en) | 2014-02-27 |
| NZ621156A (en) | 2016-01-29 |
| SG10201507001RA (en) | 2015-10-29 |
| BR112014007850A2 (pt) | 2017-04-18 |
| KR20140071474A (ko) | 2014-06-11 |
| MX2014004062A (es) | 2014-06-05 |
| CN103857679A (zh) | 2014-06-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6392436B2 (ja) | 置換された５−フルオロ−１ｈ−ピラゾロピリジン類を製造するための方法 | |
| JP6439050B2 (ja) | Ａｓｋ１阻害剤を調製するプロセス | |
| KR101501856B1 (ko) | 프로판-1-설폰산｛3-[5-(4-클로로-페닐)-1H-피롤로[2,3-b]피리딘-3-카본일]-2,4-다이플루오로-페닐｝-아마이드의 신규 제조 방법 | |
| JP6147856B2 (ja) | インテグラーゼインヒビターを調製するためのプロセスおよび中間体 | |
| JP2013047248A (ja) | インテグラーゼ阻害剤を調製するためのプロセスおよび中間体 | |
| CN107176955A (zh) | 一种巴瑞替尼的制备方法 | |
| JP2024054201A (ja) | １－［（３ｒ，４ｓ）－４－シアノテトラヒドロピラン－３－イル］－３－［（２－フルオロ－６－メトキシ－４－ピリジル）アミノ］ピラゾール－４－カルボキサミドの調製方法 | |
| WO2013097629A1 (zh) | 一种盐酸阿莫罗芬的制备方法 | |
| CN107513050B (zh) | 一种烯酸溴内酯化的制备方法 | |
| JP2021509685A (ja) | クリサボロールおよびその中間体を調製するためのプロセス | |
| RU2630700C2 (ru) | СПОСОБЫ ПОЛУЧЕНИЯ 5-[2-[7-(ТРИФТОРМЕТИЛ)-5-[4-(ТРИФТОРМЕТИЛ)ФЕНИЛ]ПИРАЗОЛО[1,5-a]ПИРИМИДИН-3-ИЛ]ЭТИНИЛ]-2-ПИРИДИНАМИНА | |
| JP6839715B2 (ja) | １−（４−メタンスルホニル−２−トリフルオロメチル−ベンジル）−２−メチル−１Ｈ−ピロロ［２，３−ｂ］ピリジン−３−イル−酢酸を調製するための方法 | |
| JP2013537534A (ja) | 化合物ｏｓｉ−９０６の調製のためのプロセス | |
| NZ621156B2 (en) | Methods for the preparation of 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine | |
| TWI845992B (zh) | 一種ｂ肝病毒核衣殼抑制劑的製備方法 | |
| JP2769058B2 (ja) | シクロプロパン誘導体の製法 | |
| HK1193603A (en) | Methods for the preparation of 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine | |
| CN111100112A (zh) | 苯并噻吩衍生物及其制备方法 | |
| JP6997769B2 (ja) | ２－（６－ニトロピリジン－３－イル）－９Ｈ－ジピリド［２，３－ｂ；３’，４’－ｄ］ピロールの製造方法 | |
| JP6216895B2 (ja) | ９−アリルカンプトセシン誘導体の合成方法 | |
| KR20170080190A (ko) | 1,5-쌍극자의 [5+3] 고리화 첨가 반응을 이용한 8원 헤테로 고리 화합물의 제조 방법 및 이에 의해 제조된 8원 헤테로 고리 화합물 | |
| CN119912431A (zh) | 一种阿贝西利杂质a的制备方法及其控制 | |
| CN117088818A (zh) | 一种4,6-二氯-2-丙硫基-5-氨基嘧啶的合成方法 | |
| KR101346555B1 (ko) | 9-히드록시-3-(2-클로로에틸)-2-메틸-6,7,8,9-테트라히드로-4Ｈ-피리도[1,2-ａ]피리미딘-4-온의 제조방법 | |
| CN121318978A (zh) | 一种他雷替尼中间体的生产工艺 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RD04 | Notification of resignation of power of attorney |
Free format text: JAPANESE INTERMEDIATE CODE: A7424 Effective date: 20150310 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150930 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20150930 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20160428 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20160524 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20160823 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20161021 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20170131 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20170530 |
|
| A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20170725 |
|
| A912 | Re-examination (zenchi) completed and case transferred to appeal board |
Free format text: JAPANESE INTERMEDIATE CODE: A912 Effective date: 20170818 |