CA2847092A1 - Methods for the preparation of 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine - Google Patents

Methods for the preparation of 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine Download PDF

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Publication number
CA2847092A1
CA2847092A1 CA2847092A CA2847092A CA2847092A1 CA 2847092 A1 CA2847092 A1 CA 2847092A1 CA 2847092 A CA2847092 A CA 2847092A CA 2847092 A CA2847092 A CA 2847092A CA 2847092 A1 CA2847092 A1 CA 2847092A1
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CA
Canada
Prior art keywords
compound
inert solvent
reacting
formula
preparing
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.)
Abandoned
Application number
CA2847092A
Other languages
English (en)
French (fr)
Inventor
Stephan Bachmann
Daniel Bailey
Jodie Brice
Miall Cedilote
Zhiming Dong
Stefan Hildbrand
Doreen Miller
Paul Spurr
Amit Srivastava
Juergen Wichmann
Thomas Woltering
Jason Yang
Pingsheng Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CA2847092A1 publication Critical patent/CA2847092A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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)
CA2847092A 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 Abandoned CA2847092A1 (en)

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 (1)

Publication Number Publication Date
CA2847092A1 true CA2847092A1 (en) 2013-04-11

Family

ID=46963723

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2847092A Abandoned CA2847092A1 (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

Country Status (15)

Country Link
US (1) US9447099B2 (https=)
EP (1) EP2763991B1 (https=)
JP (1) JP2014532058A (https=)
KR (1) KR20140071474A (https=)
CN (1) CN103857679A (https=)
AR (1) AR088098A1 (https=)
AU (1) AU2012320732A1 (https=)
BR (1) BR112014007850A2 (https=)
CA (1) CA2847092A1 (https=)
IL (1) IL231283A0 (https=)
MX (1) MX2014004062A (https=)
RU (1) RU2630700C2 (https=)
SG (2) SG2014014203A (https=)
WO (1) WO2013050310A1 (https=)
ZA (1) ZA201401398B (https=)

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
JP7167163B2 (ja) * 2019-05-20 2022-11-08 煙台邁百瑞国際生物医薬股▲ふん▼有限公司 抗体-薬物コンジュゲートの中間体のワンポット合成法による製造プロセス

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004111040A1 (en) 2003-06-12 2004-12-23 F. Hoffmann-La Roche Ag Heteroaryl-substituted imdazole derivatives as glutamate receptor antagonists
US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
DE602005014621D1 (de) * 2004-03-09 2009-07-09 Boehringer Ingelheim Pharma 3-ä4-heterocyclyl-1,2,3-triazol-1-ylü-n-arylbenzamide als inhibitoren der cytokinenproduktion für die behandlung von chronischen entzündlichen erkrankungen
CN101115755B (zh) * 2005-02-11 2013-01-16 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的吡唑并-嘧啶衍生物
DE602006012815D1 (de) * 2005-03-23 2010-04-22 Hoffmann La Roche Acetylenylpyrazolopyrimidinderivate als mglur2-antagonsten
AU2006298829B2 (en) * 2005-09-27 2011-03-03 F. Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mGluR2 antagonists
AR074231A1 (es) * 2008-11-27 2010-12-29 Boehringer Ingelheim Int Derivados de 6, 7, 8, 9-tetrahidro-5h-1, 4, 7, 10a-tetraaza-ciclohept[f]indeno, composiciones farmacéuticas que contienen estos compuestos, su uso en el agonismo del receptor 5-ht2c y procesos para prepararlos.
WO2011014520A2 (en) * 2009-07-29 2011-02-03 Irm Llc Compounds and compositions as modulators of gpr119 activity

Also Published As

Publication number Publication date
BR112014007850A2 (pt) 2017-04-18
SG10201507001RA (en) 2015-10-29
AU2012320732A1 (en) 2014-02-27
RU2014116885A (ru) 2015-11-10
RU2630700C2 (ru) 2017-09-12
CN103857679A (zh) 2014-06-11
KR20140071474A (ko) 2014-06-11
NZ621156A (en) 2016-01-29
WO2013050310A1 (en) 2013-04-11
US9447099B2 (en) 2016-09-20
EP2763991A1 (en) 2014-08-13
SG2014014203A (en) 2014-05-29
ZA201401398B (en) 2017-04-26
IL231283A0 (en) 2014-04-30
US20130085278A1 (en) 2013-04-04
AR088098A1 (es) 2014-05-07
EP2763991B1 (en) 2016-12-28
JP2014532058A (ja) 2014-12-04
MX2014004062A (es) 2014-06-05

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Date Code Title Description
EEER Examination request

Effective date: 20170929

FZDE Discontinued

Effective date: 20191001