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 PDFInfo
- 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
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- compound
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- inert solvent
- react
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- 0 CC(CC*)c(cc1)ccc1-c1nc2c(*)cn[n]2c(C(F)(F)F)c1 Chemical compound CC(CC*)c(cc1)ccc1-c1nc2c(*)cn[n]2c(C(F)(F)F)c1 0.000 description 2
- ZVGIVKMNLUTRPN-UHFFFAOYSA-N C#Cc(cc1)cnc1N Chemical compound C#Cc(cc1)cnc1N ZVGIVKMNLUTRPN-UHFFFAOYSA-N 0.000 description 1
- TUTUTUJODZAPSZ-UHFFFAOYSA-N CC(C)(C#Cc(cc1)cnc1N)O Chemical compound CC(C)(C#Cc(cc1)cnc1N)O TUTUTUJODZAPSZ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
-
- 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 (1)
| Publication Number | Publication Date |
|---|---|
| CN103857679A true CN103857679A (zh) | 2014-06-11 |
Family
ID=46963723
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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)
| 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)
| 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)
| 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 |
-
2012
- 2012-09-27 US US13/628,069 patent/US9447099B2/en not_active Expired - Fee Related
- 2012-10-01 RU RU2014116885A patent/RU2630700C2/ru not_active IP Right Cessation
- 2012-10-01 CA CA2847092A patent/CA2847092A1/en not_active Abandoned
- 2012-10-01 SG SG10201507001RA patent/SG10201507001RA/en unknown
- 2012-10-01 CN CN201280048837.2A patent/CN103857679A/zh active Pending
- 2012-10-01 AU AU2012320732A patent/AU2012320732A1/en not_active Abandoned
- 2012-10-01 SG SG2014014203A patent/SG2014014203A/en unknown
- 2012-10-01 MX MX2014004062A patent/MX2014004062A/es unknown
- 2012-10-01 EP EP12766655.0A patent/EP2763991B1/en not_active Not-in-force
- 2012-10-01 KR KR1020147011727A patent/KR20140071474A/ko not_active Ceased
- 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 JP JP2014533842A patent/JP2014532058A/ja 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 |
|---|---|---|---|---|
| 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)
| 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) * |
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 |
| 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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