CAS: 883986-34-3; 2-(4-((6,7-Dimethoxyquinazolin-4-yl)Oxy)Phenyl)-N-(1-Isopropyl-1H-Pyrazol-4-yl)Acetamide

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2-[4-(6,7-Dimethoxyquinazolin-4-Yloxy)Phenyl]Acetic Acid 883985-18-0

合成工艺路线路线简述

  • 883985-18-0 + 97421-16-4 = 883986-34-3
    反应条件:1.1 Reagents: Triethylamine,2-Hydroxypyridine N-Oxide,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; 12 H,55 °C
    标题:Discovery Of Azd2932,A New Quinazoline Ether Inhibitor With High Affinity For Vegfr-2 And Pdgfr Tyrosine Kinases
    作者:Ple,Patrick A.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2012 卷标:22(1) 页码:262-266]

    883985-18-0 + 97421-16-4 = 883986-34-3
    反应条件:1.1 Reagents: Diisopropylethylamine,2-Hydroxypyridine N-Oxide,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; 2 H,50 °C
    标题:Discovery Of New Quinoline Ether Inhibitors With High Affinity And Selectivity For Pdgfr Tyrosine Kinases
    作者:Ple,Patrick A.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2012 卷标:22(9) 页码:3050-3055]

    13790-39-1 + 156-38-7 = 883986-34-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 5 H,90 °C2.1 Reagents: Diisopropylethylamine,2-Hydroxypyridine N-Oxide,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; 2 H,50 °C
    标题:Discovery Of New Quinoline Ether Inhibitors With High Affinity And Selectivity For Pdgfr Tyrosine Kinases
    作者:Ple,Patrick A.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2012 卷标:22(9) 页码:3050-3055]

    13790-39-1 + 156-38-7 = 883986-34-3
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; 4 H,90 °C2.1 Reagents: Triethylamine,2-Hydroxypyridine N-Oxide,1-Ethyl-3-(3′-Dimethylaminopropyl)Carbodiimide Hydrochloride Solvents: Dimethylformamide; 12 H,55 °C
    标题:Discovery Of Azd2932,A New Quinazoline Ether Inhibitor With High Affinity For Vegfr-2 And Pdgfr Tyrosine Kinases
    作者:Ple,Patrick A.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2012 卷标:22(1) 页码:262-266
📜4-氯-6,7-二甲氧基喹唑啉置于potassium Carbonate,N,N-二异丙基乙胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 18.0H,反应生成 4-[(6,7-二甲氧基-4-喹唑啉)氧基]-N-[1-(1-甲基乙基)-1H-吡唑-4-基]-苯乙酰胺
参考文献:Discovery Of Azd2932,A New Quinazoline Ether Inhibitor With High Affinity For Vegfr-2 And Pdgfr Tyrosine Kinases
标题:Discovery Of Azd2932,A New Quinazoline Ether Inhibitor With High Affinity For Vegfr-2 And Pdgfr Tyrosine Kinases
摘要:A New Series Of Quinazoline Ether Inhibitor Which Potently Inhibits Vegfr-2 And Pdgfr Tyrosine Kinases Is Described Here. In Vitro,Pharmacokinetics And In Vivo Evaluations Led To The Selection Of Azd2932. (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2011.11.019

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主要参考文献


1: Plé PA, Jung F, Ashton S, Hennequin L, Laine R, Morgentin R, Pasquet G, Taylor S. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6. doi: 10.1016/j.bmcl.2011.11.019. Epub 2011 Nov 12. E., Mabrouk, R. R., Elnagar, M. R., Farrag, A. M., Kalaba, M. H., Sharaf, M. H., ... & Al Ward, M. M. S. (2023). New series of VEGFR-2 inhibitors and apoptosis enhancers: design, synthesis and biological evaluation. Drug Design, Development and Therapy, 587-606.

合成参考文献


参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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