CN103857679A - 制备5-[2-[7-(三氟甲基)-5-[4-(三氟甲基)苯基]吡唑并[1,5-a]嘧啶-3-基]乙炔基]-2-吡啶胺的方法 - Google Patents

制备5-[2-[7-(三氟甲基)-5-[4-(三氟甲基)苯基]吡唑并[1,5-a]嘧啶-3-基]乙炔基]-2-吡啶胺的方法 Download PDF

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Publication number
CN103857679A
CN103857679A CN201280048837.2A CN201280048837A CN103857679A CN 103857679 A CN103857679 A CN 103857679A CN 201280048837 A CN201280048837 A CN 201280048837A CN 103857679 A CN103857679 A CN 103857679A
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China
Prior art keywords
compound
produce
inert solvent
react
compd
Prior art date
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Pending
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CN201280048837.2A
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English (en)
Chinese (zh)
Inventor
斯蒂芬·巴赫曼
丹尼尔·贝利
乔迪·布赖斯
迈阿尔·塞德林德
董志明
斯特凡·希尔德布兰德
多琳·米勒
保罗·斯珀尔
阿米特·斯里瓦斯塔瓦
于尔根·维希曼
托马斯·沃尔特林
詹森·杨
张平生
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN103857679A publication Critical patent/CN103857679A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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)
CN201280048837.2A 2011-10-04 2012-10-01 制备5-[2-[7-(三氟甲基)-5-[4-(三氟甲基)苯基]吡唑并[1,5-a]嘧啶-3-基]乙炔基]-2-吡啶胺的方法 Pending CN103857679A (zh)

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
CN103857679A true CN103857679A (zh) 2014-06-11

Family

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Family Applications (1)

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CN201280048837.2A Pending CN103857679A (zh) 2011-10-04 2012-10-01 制备5-[2-[7-(三氟甲基)-5-[4-(三氟甲基)苯基]吡唑并[1,5-a]嘧啶-3-基]乙炔基]-2-吡啶胺的方法

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
WO2006084634A1 (en) * 2005-02-11 2006-08-17 F.Hoffmann-La Roche Ag Pyrazolo-pyrimidine derivatives as mglur2 antagonists
CN1890242A (zh) * 2003-10-03 2007-01-03 弗·哈夫曼-拉罗切有限公司 吡唑并和咪唑并-嘧啶衍生物
WO2007039439A1 (en) * 2005-09-27 2007-04-12 F.Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists
CN101180299A (zh) * 2005-03-23 2008-05-14 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的乙炔基-吡唑并嘧啶衍生物

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
CN1930144A (zh) * 2004-03-09 2007-03-14 贝林格尔·英格海姆药物公司 可用作细胞因子产生抑制剂用于治疗慢性炎性疾病的3,4’-杂环基-1,2,3-三唑-1-基-n-芳基苯甲酰胺
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1890242A (zh) * 2003-10-03 2007-01-03 弗·哈夫曼-拉罗切有限公司 吡唑并和咪唑并-嘧啶衍生物
WO2006084634A1 (en) * 2005-02-11 2006-08-17 F.Hoffmann-La Roche Ag Pyrazolo-pyrimidine derivatives as mglur2 antagonists
CN101180299A (zh) * 2005-03-23 2008-05-14 弗·哈夫曼-拉罗切有限公司 作为mglur2拮抗剂的乙炔基-吡唑并嘧啶衍生物
WO2007039439A1 (en) * 2005-09-27 2007-04-12 F.Hoffmann-La Roche Ag Oxadiazolyl pyrazolo-pyrimidines as mglur2 antagonists

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HARRI TAKALO,等: "Synthesis of some substituted dimethyl and diethyl 4-(phenylethynyl)-2,6-pyridinedicarboxylates", 《ACTA CHEMICA SCANDINAVICA B》, 31 December 1988 (1988-12-31) *
M.I.BARDAMOVA,等: "Acetylenic derivatives of anlline", 《BULLETIN OF THE ACADEMY OF SCIENCES OF THE USSR DIVISION OF CHEMICAL SCIENCE》, 31 December 1982 (1982-12-31) *

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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
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
JP2014532058A (ja) 2014-12-04
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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