CAS: 870483-87-7; 5-(3-Methoxy-4-((4-Methoxybenzyl)Oxy)Benzyl)Pyrimidine-2,4-Diamine

该化合物是一个小分子抑制器,主要以其作为聚居点刺激因子1受体(CSF1R)的选择性对抗者的作用而闻名.该化合物在癌症研究和免疫学领域引起了人们的注意,因为它有可能通过抑制大型细胞征召和激活来调节肿瘤微环境.GW2580的特征是它能够干扰CSF1信号路径,这对大型植物的生存和扩散至关重要.该化合物通常在临床前模型中研究,以评价其在各种癌症类型和炎热性疾病中的功效.就其化学特性而言,GW2580是一种合成化合物,具有特定的分子结构,使其能够有选择地与CSF1R结合,从而阻止其活动.它的药理学学特征,包括吸收,分布,新陈代谢和排泄(ADME),也是其发展成为治疗剂的重要考虑因素.

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合成工艺路线路线简述

  • 824-94-2 + 121-33-5 = 870483-87-7
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; Rt; 3 H,70 °C2.1 Solvents: Dimethyl Sulfoxide; 65 °C; 65 °C -> 40 °C2.2 Reagents: Sodium Methoxide Solvents: Methanol; 15 - 25 Min,75 °C3.1 Solvents: Isopropanol; 20 Min,Reflux4.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 12 H,Reflux; Reflux -> 5 °C4.2 Reagents: Sodium Hydroxide Solvents: Water
    标题:5-(4-((4-[18F]Fluorobenzyl)Oxy)-3-Methoxybenzyl)Pyrimidine-2,4-Diamine: A Selective Dual Inhibitor For Potential Pet Imaging Of Trk/csf-1R
    作者:Bernard-Gauthier,Vadim; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2014 卷标:24(20) 页码:4784-4790]

    50-01-1 + 1227960-77-1 = 870483-87-7
    反应条件:1.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 12 H,Reflux; Reflux -> 5 °C1.2 Reagents: Sodium Hydroxide Solvents: Water
    标题:5-(4-((4-[18F]Fluorobenzyl)Oxy)-3-Methoxybenzyl)Pyrimidine-2,4-Diamine: A Selective Dual Inhibitor For Potential Pet Imaging Of Trk/csf-1R
    作者:Bernard-Gauthier,Vadim; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2014 卷标:24(20) 页码:4784-4790]

    = 870483-87-7
    反应条件:1.1 Solvents: Isopropanol; 20 Min,Reflux2.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 12 H,Reflux; Reflux -> 5 °C2.2 Reagents: Sodium Hydroxide Solvents: Water
    标题:5-(4-((4-[18F]Fluorobenzyl)Oxy)-3-Methoxybenzyl)Pyrimidine-2,4-Diamine: A Selective Dual Inhibitor For Potential Pet Imaging Of Trk/csf-1R
    作者:Bernard-Gauthier,Vadim; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2014 卷标:24(20) 页码:4784-4790]

    4542-47-6 + 129047-38-7 = 870483-87-7
    反应条件:1.1 Solvents: Dimethyl Sulfoxide; 65 °C; 65 °C -> 40 °C1.2 Reagents: Sodium Methoxide Solvents: Methanol; 15 - 25 Min,75 °C2.1 Solvents: Isopropanol; 20 Min,Reflux3.1 Reagents: Sodium Ethoxide Solvents: Ethanol; 12 H,Reflux; Reflux -> 5 °C3.2 Reagents: Sodium Hydroxide Solvents: Water
    标题:5-(4-((4-[18F]Fluorobenzyl)Oxy)-3-Methoxybenzyl)Pyrimidine-2,4-Diamine: A Selective Dual Inhibitor For Potential Pet Imaging Of Trk/csf-1R
    作者:Bernard-Gauthier,Vadim; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2014 卷标:24(20) 页码:4784-4790
📜盐酸胍,3-Anilino-2-{3-Methoxy-4-[(4-Methoxybenzyl)Oxy]Benzyl}Prop-2-Enenitrile置于sodium Methylate体系中,用 乙醇 作为反应溶剂,化学反应生成 5-[[3-甲氧基-4-[(4-甲氧基苯基)甲氧基]苯基]甲基]-2,4-嘧啶二胺',
参考文献:Crystal Structure Of Liganded Cfms Kinase Domain
标题:Crystal Structure Of Liganded Cfms Kinase Domain
摘要:Cfms激酶结构的晶体结构,与一个结合的小分子的共晶结构,以及使用相同方法在发现cfms抑制剂和治疗由不当cfms活性介导的疾病中的应用.

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专利信息


专利号:CN-108379591-B
优先权日:2018-04-03
标 题 :Synthesis of Immune Agonist Targeting Compounds and Their Applications

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主要参考文献


1: Weizman N, Krelin Y, Shabtay-Orbach A, Amit M, Binenbaum Y, Wong RJ, Gil Z. Macrophages mediate gemcitabine resistance of pancreatic adenocarcinoma by upregulating cytidine deaminase. Oncogene. 2013 Sep 2. doi: 10.1038/onc.2013.357. [Epub ahead of print] doi: 10.1016/j.cyto.2013.04.019. Epub 2013 May 14. doi: 10.1371/journal.pone.0054302. Epub 2013 Jan 23.
4: Komohara Y, Horlad H, Ohnishi K, Fujiwara Y, Bai B, Nakagawa T, Suzu S, Nakamura H, Kuratsu J, Takeya M. Importance of direct macrophage-tumor cell interaction on progression of human glioma. Cancer Sci. 2012 Dec;103(12):2165-72. doi: 10.1111/cas.12015. Epub 2012 Oct 26. doi: 10.1016/j.cyto.2012.03.029. Epub 2012 Apr 18. doi: 10.1002/glia.22291. Epub 2012 Jan 18. doi: 10.1093/jb/mvr112. Epub 2011 Aug 31. doi: 10.1177/1087057111418113. Epub 2011 Aug 26. doi: 10.1007/s10875-011-9579-6. Epub 2011 Aug 17.
10: Eda H, Zhang J, Keith RH, Michener M, Beidler DR, Monahan JB. Macrophage-colony stimulating factor and interleukin-34 induce chemokines in human whole blood. Cytokine. 2010 Dec;52(3):215-20. doi: 10.1016/j.cyto.2010.08.005. Epub 2010 Sep 9. doi: 10.1158/0008-5472.CAN-10-0522. Epub 2010 Sep 7.

合成参考文献


参考文献:10.1021/acs.jmedchem.0c00936
摘要:Czako B, Marszalek JR, Burke JP, Mandal P, Leonard PG, Cross JB, Mseeh F, Jiang Y, Chang EQ, Suzuki E, Kovacs JJ, Feng N, Gera S, Harris AL, Liu Z, Mullinax RA, Pang J, Parker CA, Spencer ND, Yu SS, Wu Q, Tremblay MR, Mikule K, Wilcoxen K, Heffernan TP, Draetta GF, Jones P. Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R. J Med Chem. 2020 Sep 10;63(17):9888–911. doi: 10.1021/acs.jmedchem.0c00936.
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