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

    • 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)
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 (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)

* Cited by examiner, † Cited by third party
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
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
EP1725544B1 (en) * 2004-03-09 2009-05-27 Boehringer Ingelheim Pharmaceuticals Inc. 3-[4-heterocyclyl-1,2,3-triazol-1-yl]-n-aryl-benzamides as inhibitors of the cytokines production for the treatment of chronic inflammatory diseases
ATE512966T1 (de) * 2005-02-11 2011-07-15 Hoffmann La Roche Pyrazolo-pyrimidin-derivate als mglur2- antagonisten
PT1863818E (pt) * 2005-03-23 2010-04-09 Hoffmann La Roche Derivados de acetilenil-pirazolo-pirimidina como antagonistas de mglur2
ATE463495T1 (de) * 2005-09-27 2010-04-15 Hoffmann La Roche Oxadiazolylpyrazolopyrimidine als mglur2- antagonisten
EP2384328B1 (en) * 2008-11-27 2013-02-13 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 process for preparing them
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
RU2630700C2 (ru) 2017-09-12
US20130085278A1 (en) 2013-04-04
RU2014116885A (ru) 2015-11-10
ZA201401398B (en) 2017-04-26
AR088098A1 (es) 2014-05-07
SG2014014203A (en) 2014-05-29
JP2014532058A (ja) 2014-12-04
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

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Date Code Title Description
EEER Examination request

Effective date: 20170929

FZDE Discontinued

Effective date: 20191001