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 PDF

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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
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compound
providing
inert solvent
producing
reacting
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JP2014533842A
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Japanese (ja)
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JP2014532058A5 (enExample
Inventor
バッハマン,シュテファン
ベイリー,ダニエル
ブライス,ジョディ
セディロート,マイアル
ドン,ジーミン
ヒルトブラント,シュテファン
ミラー,ドリーン
シュプール,ポール
スリヴァスタヴァ,アミット
ヴィッヒマン,ユルゲン
ヴォルテリング,トーマス
ヤン,ジェイソン
ツァン,ピンシェン
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of JP2014532058A publication Critical patent/JP2014532058A/ja
Publication of JP2014532058A5 publication Critical patent/JP2014532058A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/081Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0803Compounds with Si-C or Si-Si linkages
    • C07F7/0825Preparations of compounds not comprising Si-Si or Si-cyano linkages
    • C07F7/083Syntheses without formation of a Si-C bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/73Unsubstituted amino or imino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2014533842A 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 Pending JP2014532058A (ja)

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) SG10201507001RA (enExample)
WO (1) WO2013050310A1 (enExample)
ZA (1) ZA201401398B (enExample)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20160143853A (ko) * 2014-04-23 2016-12-14 에프. 호프만-라 로슈 아게 지적 장애의 치료를 위한 mglu2/3 길항제
EP3760233B1 (en) * 2019-05-20 2023-07-12 MabPlex International Co., Ltd. One-pot preparation process for antibody drug conjugate intermediate

Citations (4)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE495168T1 (de) 2003-06-12 2011-01-15 Hoffmann La Roche Heteroarylsubstituierte imidazolderivate als glutamatrezeptorantagonisten
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
ES2365406T3 (es) * 2005-02-11 2011-10-04 F. Hoffmann-La Roche Ag Derivados de pirazolo-pirimidina como antagonistas de mglur2.
CA2623721C (en) * 2005-09-27 2014-05-13 F. Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists

Patent Citations (4)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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
MX2014004062A (es) 2014-06-05
US9447099B2 (en) 2016-09-20
EP2763991B1 (en) 2016-12-28
IL231283A0 (en) 2014-04-30
NZ621156A (en) 2016-01-29
CN103857679A (zh) 2014-06-11
ZA201401398B (en) 2017-04-26
SG2014014203A (en) 2014-05-29
CA2847092A1 (en) 2013-04-11
EP2763991A1 (en) 2014-08-13
AU2012320732A1 (en) 2014-02-27
AR088098A1 (es) 2014-05-07
BR112014007850A2 (pt) 2017-04-18
KR20140071474A (ko) 2014-06-11
WO2013050310A1 (en) 2013-04-11
US20130085278A1 (en) 2013-04-04
SG10201507001RA (en) 2015-10-29
RU2014116885A (ru) 2015-11-10
RU2630700C2 (ru) 2017-09-12

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