CAS: 872511-34-7; 3-(2,6-Dichloro-3,5-Dimethoxyphenyl)-1-(6-((4-(4-Ethylpiperazin-1-yl)Phenyl)Amino)Pyrimidin-4-yl)-1-Methylurea

该化合物是合成有机化合物,属于尿素衍生物类别,具有多种功能组的复杂分子结构,包括尿素,芳香环和卤素替代体.二氯和甲氧氧基化合物的存在表明潜在的生物活动,可能影响其药理特性.该化合物经常在药用化学中研究其潜在用途,特别是针对特定生物途径或受体.其复杂结构可能有助于其溶解性,稳定性和与生物系统的互动.与许多合成化合物一样,了解其特性,包括其耐受性,溶性以及潜在毒性,对于评价其是否适合治疗用途至关重要.在相关背景下,需要进一步研究,以阐明其行动机制和相关生物功效.

结构式图片

物理性质

MSDS等安全信息

上下游产品

2,4-dichloro-3-is°Cyanato-1,5-methoxy-4-methylbenzene 4-(4-(4-ethylpiperazin-1-yl)phenyl)-N6-methylpyrimidine-4,6-diamineof N4-(4-(4-ethylpiperazin-1-yl)phenyl)-N6-methylpyrimidine-4,6-diamine

合成工艺路线路线简述

  • 872509-56-3 + 872511-35-8 = 872511-34-7
    反应条件:1.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt1.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    115619-01-7 + 65766-32-7 = 872511-34-7
    反应条件:1.1 Reagents: Acetic Acid Solvents: Water; 16 H,Rt -> 100 °C; 24 H,100 °C; Cooled1.2 Reagents: Sodium Bicarbonate Solvents: Water; Basified,Cooled2.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt2.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    943189-21-7 = 872511-34-7
    反应条件:1.1 Reagents: Potassium Hydroxide Solvents: Ethanol,Water; 44 H,Rt -> Reflux2.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt2.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    115619-00-6 = 872511-34-7
    反应条件:1.1 Reagents: Hydrogen Catalysts: Nickel Solvents: Methanol; 7 H,Rt2.1 Reagents: Acetic Acid Solvents: Water; 16 H,Rt -> 100 °C; 24 H,100 °C; Cooled2.2 Reagents: Sodium Bicarbonate Solvents: Water; Basified,Cooled3.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt3.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    1193-21-1 = 872511-34-7
    反应条件:1.1 Solvents: Ethanol,Isopropanol; 50 °C; 1 H,Rt2.1 Reagents: Acetic Acid Solvents: Water; 16 H,Rt -> 100 °C; 24 H,100 °C; Cooled2.2 Reagents: Sodium Bicarbonate Solvents: Water; Basified,Cooled3.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt3.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    79257-61-7 = 872511-34-7
    反应条件:1.1 Reagents: Sulfuryl Chloride Solvents: Acetonitrile; 7 Min,0 °C; 30 Min,0 °C1.2 Reagents: Sodium Bicarbonate Solvents: Water; 0 °C2.1 Reagents: Potassium Hydroxide Solvents: Ethanol,Water; 44 H,Rt -> Reflux3.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt3.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    10272-07-8 = 872511-34-7
    反应条件:1.1 Solvents: Toluene; 15 Min,35 - 45 °C; 20 H,Rt2.1 Reagents: Sulfuryl Chloride Solvents: Acetonitrile; 7 Min,0 °C; 30 Min,0 °C2.2 Reagents: Sodium Bicarbonate Solvents: Water; 0 °C3.1 Reagents: Potassium Hydroxide Solvents: Ethanol,Water; 44 H,Rt -> Reflux4.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt4.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083]

    5308-25-8 = 872511-34-7
    反应条件:1.1 15 H,Rt -> 80 °C2.1 Reagents: Hydrogen Catalysts: Nickel Solvents: Methanol; 7 H,Rt3.1 Reagents: Acetic Acid Solvents: Water; 16 H,Rt -> 100 °C; 24 H,100 °C; Cooled3.2 Reagents: Sodium Bicarbonate Solvents: Water; Basified,Cooled4.1 Solvents: Toluene,1,4-Dioxane; 1 H,Rt -> Reflux; Reflux -> Rt4.2 Solvents: Toluene; Rt; 1.5 H,Rt -> Reflux
    标题:Discovery Of 3-(2,6-Dichloro-3,5-Dimethoxy-Phenyl)-1-{6-[4-(4-Ethyl-Piperazin-1-Yl)-Phenylamino]-Pyrimidin-4-Yl}-1-Methyl-Urea (Nvp-Bgj398),A Potent And Selective Inhibitor Of The Fibroblast Growth Factor Receptor Family Of Receptor Tyrosine Kinase
    作者:Guagnano,Vito; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(20) 页码:7066-7083
4-(4-乙基哌嗪-1-基)苯胺置于盐酸体系中,用 1,4-二氧六环,甲苯 作为反应溶剂,化学反应 6.5H,反应生成 Fgfr抑制剂(Nvp-Bgj398)
参考文献: Methods Of Treating Achondroplasia[fr] Méthodes De Traitement De L'Achondroplasie
标题: Methods Of Treating Achondroplasia[fr] Méthodes De Traitement De L'Achondroplasie
摘要:Provided Herein Are Methods Of Treating A Skeletal Dysplasia Such As Hypochondroplasia Or Achondroplasia In A Pediatric Patient By Administering To The Patient Infigratinib Or A Pharmaceutically Acceptable Salt Thereof. Also Provided Are Minitablets Including Infigratinib Monophosphate And A Pharmaceutically Acceptable Excipient For Use In Treating A Skeletal Dysplasia Such As Hypochondroplasia Or Achondroplasia In Pediatric Patients.

海关参考信息

专利信息


专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-12390420-B1
优先权日:2024-10-22
标题 :Compositions for targeted delivery of therapeutic agents and methods for the synthesis and use thereof
发明人：EGUCHI MASAKATSU
权利人:BRYET US INC
摘要:The present disclosure provides compositions and methods for delivering therapeutic agents to particular tissues or cells in a subject. The composition disclosed herein combines unique properties of porous micro- or nano-particles with host-guest chemistry provided by functionalized silicon particle, offering a versatile approach to addressing the challenges associated with delivering therapeutic agents to target tissues or sites within the body. The present disclosure also provides a method for synthesizing a composition capable of delivering therapeutic agents to particular tissues or cells in a subject.

专利号:US-2024066133-A1
优先权日:2020-03-06
标 题 :Therapeutic agents and conjugates thereof
发明人：SONG YUNTAO; LI ANRONG; LI HUI; LI XIANFENG; YANG JUNBAO
权利人:BEIJING XUANYI PHARMASCIENCES CO LTD
摘要:The present disclosure provides a class of conjugates of general formula (X), a class of TLR9 agonist derivatives, such as formula (I), (XX), and (XXI), certain diastereomers of STING agonists, a class of STING agonist derivatives, such as formula (XXVIV), a class of heterocyclic compounds of general formula (II), a class of heterocyclic compounds of general formula (III), as defined herein. A 1 , A 2 , T, Z 1 , Z 2 , Z 3 , b 1 , and b 2 , in formula (X) are defined herein. The conjugate provides unique properties that are based upon the properties of the therapeutic agents that are part of the conjugate. Also provided are methods of synthesis and use of compounds.

专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人：WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.

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主要参考文献


1: Tran A, Koh TS, Prawira A, Ho RZW, Le TBU, Vu TC, Hartano S, Teo XQ, Chen WC, Lee P, Thng CH, Huynh H. Dynamic Contrast-Enhanced Magnetic Resonance Imaging as Imaging Biomarker for Vascular Normalization Effect of Infigratinib in High- FGFR-Expressing Hepatocellular Carcinoma Xenografts. Mol Imaging Biol. 2020 Sep 9. doi: 10.1007/s11307-020-01531-7. Epub ahead of print. 126(11):2597-2606. doi: 10.1002/cncr.32806. Epub 2020 Mar 24.
6: Felix NS, de Mendonça L, Braga CL, da Silva JS, Samary CDS, Vieira JB, Cruz F, Rocha NN, Zapata-Sudo G, Rocco PRM, Silva PL. Effects of the FGF receptor-1 inhibitor, infigratinib, with or without sildenafil, in experimental pulmonary arterial hypertension. Br J Pharmacol. 2019 Dec;176(23):4462-4473. doi: 10.1111/bph.14807. Epub 2019 Dec 5.
7: Huynh H, Lee LY, Goh KY, Ong R, Hao HX, Huang A, Wang Y, Graus Porta D, Chow P, Chung A. Infigratinib Mediates Vascular Normalization, Impairs Metastasis, and Improves Chemotherapy in Hepatocellular Carcinoma. Hepatology. 2019 Mar;69(3):943-958. doi: 10.1002/hep.30481.

合成参考文献


参考文献:10.1007/s11912-015-0477-6
摘要:Abbosh PH, McConkey DJ, Plimack ER. Targeting Signaling Transduction Pathways in Bladder Cancer. Curr Oncol Rep. 2015 Dec;17(12):58. doi: 10.1007/s11912-015-0477-6.
参考文献:10.1002/hep.30069
摘要:Ilyas SI, Gores GJ. Fibroblast Growth Factor Receptor Inhibition for Cholangiocarcinoma: Looking Through a Door Half-Opened. Hepatology. 2018 Dec;68(6):2428–30.
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