CN102471287A - 2-氨基-5-三氟甲基嘧啶衍生物的区域选择性制备方法 - Google Patents

2-氨基-5-三氟甲基嘧啶衍生物的区域选择性制备方法 Download PDF

Info

Publication number
CN102471287A
CN102471287A CN2010800346368A CN201080034636A CN102471287A CN 102471287 A CN102471287 A CN 102471287A CN 2010800346368 A CN2010800346368 A CN 2010800346368A CN 201080034636 A CN201080034636 A CN 201080034636A CN 102471287 A CN102471287 A CN 102471287A
Authority
CN
China
Prior art keywords
formula
reaction
compound
group
groups
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.)
Pending
Application number
CN2010800346368A
Other languages
English (en)
Chinese (zh)
Inventor
G.林茨
G.克雷默
S.库斯罗
J.施诺贝尔特
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.)
Boehringer Ingelheim International GmbH
Original Assignee
Boehringer Ingelheim International GmbH
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42712695&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102471287(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of CN102471287A publication Critical patent/CN102471287A/zh
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN2010800346368A 2009-08-14 2010-08-13 2-氨基-5-三氟甲基嘧啶衍生物的区域选择性制备方法 Pending CN102471287A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09167934 2009-08-14
EP09167934.0 2009-08-14
PCT/EP2010/061840 WO2011018518A1 (en) 2009-08-14 2010-08-13 Regioselective preparation of 2 -amino-5-trifluoromethylpyrimidine derivatives

Publications (1)

Publication Number Publication Date
CN102471287A true CN102471287A (zh) 2012-05-23

Family

ID=42712695

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800346368A Pending CN102471287A (zh) 2009-08-14 2010-08-13 2-氨基-5-三氟甲基嘧啶衍生物的区域选择性制备方法

Country Status (17)

Country Link
US (1) US8933227B2 (enExample)
EP (1) EP2464634B1 (enExample)
JP (1) JP5539519B2 (enExample)
KR (1) KR20120046248A (enExample)
CN (1) CN102471287A (enExample)
AR (1) AR077925A1 (enExample)
AU (1) AU2010283713A1 (enExample)
BR (1) BR112012002971A2 (enExample)
CA (1) CA2767965A1 (enExample)
CL (1) CL2012000278A1 (enExample)
EA (1) EA201200282A1 (enExample)
IL (1) IL217112A0 (enExample)
IN (1) IN2012DN01342A (enExample)
MX (1) MX2012001469A (enExample)
NZ (1) NZ597538A (enExample)
TW (1) TW201124385A (enExample)
WO (1) WO2011018518A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887860A (zh) * 2012-09-29 2013-01-23 上海泰坦科技有限公司 4-氯-6-三氟甲基嘧啶类化合物的制备方法

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY31714A (es) * 2008-03-20 2009-11-10 Boehringer Ingelheim Int Preparación selectiva de pirimidinas sustituidas
US8372974B2 (en) * 2008-03-20 2013-02-12 Boehringer Ingelheim International Gmbh Regioselective preparation of substituted pyrimidines
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
JP6391985B2 (ja) * 2014-05-16 2018-09-19 東ソー・ファインケム株式会社 ２−置換−４−（２，２，２−トリフルオロエトキシ）−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
JP6391988B2 (ja) * 2014-05-21 2018-09-19 東ソー・ファインケム株式会社 ５−（トリフルオロメチル）ピリミジン誘導体の製造方法及び新規５−（トリフルオロメチル）ピリミジン誘導体
JP6262079B2 (ja) * 2014-06-02 2018-01-17 東ソー・ファインケム株式会社 ４−（２，２，２−トリフルオロエトキシ）−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法
JP6431294B2 (ja) * 2014-06-16 2018-11-28 東ソー・ファインケム株式会社 ５−（トリフルオロメチル）ピリミジン誘導体及びその製造法
JP6479486B2 (ja) * 2015-01-16 2019-03-06 東ソー・ファインケム株式会社 ４−アルコキシ−５−（トリフルオロメチル）ピリミジン誘導体及びその製造方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2008071587A2 (en) * 2006-12-13 2008-06-19 F. Hoffmann-La Roche Ag 2-(piperidin-4-yl)-4-phenoxy- or phenylamino-pyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors
CN100465164C (zh) * 2003-09-05 2009-03-04 辉瑞产品公司 Cf3－取代嘧啶的选择性合成

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6262A (ja) 1986-03-05 1987-01-06 Ishihara Sangyo Kaisha Ltd ベンゾイルウレア系化合物の製造方法
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
PT1438053E (pt) 2001-10-17 2008-09-25 Boehringer Ingelheim Int Derivados de pirimidina, medicamento contendo estes compostos, sua utilização e processo para a sua preparação
DE10161763A1 (de) 2001-12-15 2003-07-17 Bayer Cropsience Ltd Neues herbizides Verfahren
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades dependientes de la cinasa de proteina
BR0316680A (pt) 2002-11-28 2005-10-18 Schering Ag Pirimidinas inibidoras de chk, pdk e akt, sua produção e uso como agentes farmacêuticos
EP1625121B1 (en) 2002-12-20 2010-02-24 Pfizer Products Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
AU2004272288B2 (en) 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
EP1751143A1 (en) 2004-05-14 2007-02-14 Pfizer Products Incorporated Pyrimidine derivatives for the treatment of abnormal cell growth
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
US7601714B2 (en) 2004-07-08 2009-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Pyrimidine derivatives useful as inhibitors of PKC-theta
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
US7323447B2 (en) 2005-02-08 2008-01-29 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
EP1705177A1 (en) 2005-03-23 2006-09-27 Schering Aktiengesellschaft N-aryl-sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents
JP2008540391A (ja) 2005-05-05 2008-11-20 アストラゼネカ アクチボラグ ピラゾリルアミノ置換ピリミジン、および癌の処置におけるそれらの使用
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
TW200800963A (en) 2005-10-28 2008-01-01 Astrazeneca Ab Chemical compounds
US8722884B2 (en) 2005-12-01 2014-05-13 Verastem, Inc. Pyrimidine derivatives for the treatment of abnormal cell growth
EA014551B1 (ru) 2005-12-21 2010-12-30 Пфайзер Продактс Инк. Пиримидиновые производные для лечения аномального клеточного роста
TW200804364A (en) 2006-02-22 2008-01-16 Boehringer Ingelheim Int New compounds
JP2009533378A (ja) 2006-04-10 2009-09-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ２，４−ジアミノピリミジン誘導体及び癌の治療のためのそれらの使用
PE20120006A1 (es) 2006-05-15 2012-02-02 Boehringer Ingelheim Int Compuestos derivados de pirimidina como inhibidores de la quinasa aurora
JP5301431B2 (ja) 2006-05-18 2013-09-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング キラルな環状β−アミノカルボキサミドの製造方法
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
US8258129B2 (en) 2006-07-06 2012-09-04 Boehringer Ingelheim International Gmbh 4-heterocycloalkylpyri(mi)dines, process for the preparation thereof and their use as medicaments
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
WO2008040951A1 (en) 2006-10-03 2008-04-10 Astrazeneca Ab Compounds
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
WO2008046216A1 (en) 2006-10-18 2008-04-24 Methylgene, Inc. Kinase inhibitors and uses thereof
CA2666762C (en) 2006-10-19 2014-12-30 F. Hoffmann-La Roche Ag Aminomethyl-4-imidazoles
ES2633318T3 (es) 2006-10-23 2017-09-20 Cephalon, Inc. Derivados bicíclicos fusionados de 2,4-diaminopirimidina como inhibidores de ALK y c-Met
EP2099771A1 (en) 2006-12-19 2009-09-16 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
NZ577798A (en) 2006-12-21 2012-04-27 Vertex Pharma 5-cyano-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors
US20100144706A1 (en) 2006-12-22 2010-06-10 Boehringer Ingelheim International Gmbh Compounds
AR065015A1 (es) 2007-01-26 2009-05-13 Smithkline Beecham Corp Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2593486T3 (es) 2007-04-18 2016-12-09 Pfizer Products Inc. Derivados de sulfonil amida para el tratamiento del crecimiento celular anómalo
EP2183225A1 (en) 2007-07-17 2010-05-12 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
KR101174201B1 (ko) 2007-08-28 2012-08-16 아이알엠 엘엘씨 키나제 억제제로서의 2-비페닐아미노-4-아미노피리미딘 유도체
WO2009063240A1 (en) 2007-11-16 2009-05-22 Arrow Therapeutics Limited 2,4-diaminopyrimidine derivatives useful as inhibitors of aurora kinase
JP2011505407A (ja) 2007-12-03 2011-02-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 過剰な又は異常な細胞増殖を特徴とする疾患を治療するためのジアミノピリジン
EP2220091B1 (en) 2007-12-14 2012-07-25 Ardea Biosciences, Inc. Reverse transcriptase inhibitors
UY31714A (es) 2008-03-20 2009-11-10 Boehringer Ingelheim Int Preparación selectiva de pirimidinas sustituidas
US8372974B2 (en) 2008-03-20 2013-02-12 Boehringer Ingelheim International Gmbh Regioselective preparation of substituted pyrimidines
CN102203083A (zh) 2008-06-25 2011-09-28 Irm责任有限公司 作为激酶抑制剂的嘧啶衍生物
PE20100087A1 (es) 2008-06-25 2010-02-08 Irm Llc Compuestos y composiciones como inhibidores de cinasa
US8450335B2 (en) 2008-06-27 2013-05-28 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP2179991A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
EP2179992A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfonsubstituierte Anlinopyrimidinderivative als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
UY32240A (es) 2008-11-14 2010-06-30 Boeringer Ingelheim Kg Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones.
TW201024281A (en) 2008-11-24 2010-07-01 Boehringer Ingelheim Int New compounds
AR074210A1 (es) 2008-11-24 2010-12-29 Boehringer Ingelheim Int Derivados de pirimidina como inhibidores de ptk2-quinasa
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
WO2011018517A1 (en) 2009-08-14 2011-02-17 Boehringer Ingelheim International Gmbh Regioselective preparation of 2-amino-5-trifluoromethylpyrimidine derivatives

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003030909A1 (en) * 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
CN100465164C (zh) * 2003-09-05 2009-03-04 辉瑞产品公司 Cf3－取代嘧啶的选择性合成
WO2008071587A2 (en) * 2006-12-13 2008-06-19 F. Hoffmann-La Roche Ag 2-(piperidin-4-yl)-4-phenoxy- or phenylamino-pyrimidine derivatives as non-nucleoside reverse transcriptase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
HEINO DIRINGER,等: "Fluorinated Pyrimidines. XXXVI. Synthesis of Some 2,4-Substituted 5-Trifluoromethylpyrimidines", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 13, no. 1, 31 January 1970 (1970-01-31), pages 151 - 152, XP002304586, DOI: doi:10.1021/jm00295a047 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102887860A (zh) * 2012-09-29 2013-01-23 上海泰坦科技有限公司 4-氯-6-三氟甲基嘧啶类化合物的制备方法
CN102887860B (zh) * 2012-09-29 2015-07-01 上海泰坦科技有限公司 4-氯-6-三氟甲基嘧啶类化合物的制备方法

Also Published As

Publication number Publication date
US8933227B2 (en) 2015-01-13
JP5539519B2 (ja) 2014-07-02
US20110190499A1 (en) 2011-08-04
JP2013501759A (ja) 2013-01-17
BR112012002971A2 (pt) 2015-10-13
CA2767965A1 (en) 2011-02-17
MX2012001469A (es) 2012-02-22
IL217112A0 (en) 2012-02-29
EA201200282A1 (ru) 2012-09-28
NZ597538A (en) 2014-05-30
WO2011018518A1 (en) 2011-02-17
AU2010283713A1 (en) 2012-02-02
EP2464634B1 (en) 2016-11-30
CL2012000278A1 (es) 2012-10-12
AR077925A1 (es) 2011-10-05
KR20120046248A (ko) 2012-05-09
EP2464634A1 (en) 2012-06-20
IN2012DN01342A (enExample) 2015-06-05
TW201124385A (en) 2011-07-16

Similar Documents

Publication Publication Date Title
CN102471287A (zh) 2-氨基-5-三氟甲基嘧啶衍生物的区域选择性制备方法
CN101970416B (zh) 制备喹唑啉酮衍生物的方法
JP5104893B2 (ja) ジアミノピリミジンカルボキサミド誘導体
US8372974B2 (en) Regioselective preparation of substituted pyrimidines
EP1470121A1 (en) Pyrimidine derivatives as rho-kinase inhibitors
UA73762C2 (uk) Піримідинові сполуки, спосіб їх одержання, фармацевтична композиція та їх використання
CN101522642A (zh) 在奎宁环或n-甲基吡咯烷衍生物的存在下制备6-苯氧基嘧啶-4-醇衍生物的方法
CN101528700A (zh) 用于制备伊马替尼的方法及其中间体
US20130079519A1 (en) Regioselective preparation of substituted pyrimidines
JP5539518B2 (ja) ２−アミノ−５−トリフルオロメチルピリミジン誘導体の位置選択的調製
CN102711474B (zh) 喹唑啉化合物
CA2307770A1 (en) Novel carboxylic acid derivatives which carry amide side chains, production of said carboxylic acid derivatives and their use as endothelin receptor antagonists
CN116348450A (zh) 用于组蛋白赖氨酸去甲基化酶抑制的化合物、组合物和方法
US8093384B2 (en) Processes for the preparation of alfuzosin
JP2008266237A (ja) 環状アミン誘導体又はその塩からなる医薬

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20120523