CAS: 956034-06-3; Furo[3,2-D]Pyrimidine-2,4-Diol

该化合物是一种杂交环化合物,其特点是一个纤维化的呋喃和环系统,其独特的结构具有显著的化学特性,使其成为制药和农用化学研究的宝贵中间体; 氢氧基组在2和4个位置的存在增强了其回活动性,为生物活性衍生物合成的进一步功能化提供了便利; 该复合物作为针对特定酶道开发抑制剂或调节器的支架具有潜力; 它在标准条件下的稳定及其与共同合成方法的兼容性进一步强调了其在药用化学和材料科学应用中的实用性.

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62208-68-8 655255-08-6 1895927-78-2

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CAS号956034-07-4 2,4-二氯呋喃并[3,2-D]嘧啶 | CAS号956034-08-5 2-氯-4-吗啉呋喃并[3,2-d]嘧啶

合成工艺路线路线简述

  • 1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: Tetrahydrofuran,Water; 3.5 H,70 °C
    标题:Preparation Of Fused Heterocyclic Compound Derivative As Parp-1/pi3K Dual-Target Inhibitor And Used For The Treatment Of Tumors
    参考文献:China]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: Tetrahydrofuran; 3.5 H,70 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 6
    标题:Discovery Of Novel And Potent Parp/pi3K Dual Inhibitors For The Treatment Of Cancer
    作者:Wu,Zhengyang; Bai,Ying; Jin,Jiaming; Jiang,Teng; Shen,Hui; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2021 卷标:217]

    956034-05-2 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Water; 90 Min,Rt -> Reflux; Reflux -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 3
    标题:Thienopyrimidine And Furopyrimidine Derivatives As Phosphoinositide 3-Kinase Inhibitor And Their Preparation,Pharmaceutical Compositions And Use In The Treatment Of Cancer
    参考文献:World Intellectual Property Organization]

    956034-04-1 + 1189-71-5 = 956034-06-3
    反应条件:1.1 Solvents: Dichloromethane; -78 °C; -78 °C -> Rt; 40 Min,Rt1.2 Reagents: Sodium Bicarbonate Solvents: Water; Neutralized,Rt1.3 Reagents: Sodium Hydroxide Solvents: Methanol; 90 Min,Rt -> Reflux; Reflux -> Rt1.4 Reagents: Hydrochloric Acid Solvents: Water; Ph 3
    标题:Rational Design Of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity Over The Phosphoinositide 3-Kinase β Isoform
    作者:Heffron,Timothy P.; Wei,Bin Qing; Olivero,Alan; Staben,Steven T.; Tsui,Vickie; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2011 卷标:54(22) 页码:7815-7833]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Potassium Tert-Butoxide Solvents: Tetrahydrofuran; 1 H,Rt
    标题:Preparation Of Furanopyrimidines As Inhibitors Of Phosphatidylinositol 3-Kinase
    参考文献:World Intellectual Property Organization]

    956034-04-1 + 1189-71-5 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide,Hydrochloric Acid Solvents: Dichloromethane,Water
    标题:Identification Of 2,4-Diamino-6,7-Dimethoxyquinoline Derivatives As G9A Inhibitors
    作者:Srimongkolpithak,Nitipol; Sundriyal,Sandeep; Li,Fengling; Vedadi,Masoud; Fuchter,Matthew J.
    参考文献:Medchemcomm 日期:2014 卷标:5(12) 页码:1821-1828]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water; 90 Min,Rt -> Reflux; Reflux -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 3,Rt
    标题:Preparation Of 4-Morpholinothienopyrimidine And 4-Morpholinofuropyrimidine Derivatives As Phosphoinositide 3-Kinase Inhibitors
    参考文献:World Intellectual Property Organization]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water; 90 Min,Rt -> Reflux; Reflux -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 3,Rt
    标题:Preparation Of Thienopyrimidines And Furopyrimidines As Lipid Kinase Inhibitors For Treating Cancer And Other Diseases
    参考文献:World Intellectual Property Organization]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water; Rt -> Reflux; 90 Min,Reflux; Reflux -> Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 3
    标题:Preparation Of 4-(Morpholino)Thienopyrimidines And 4-(Morpholino)Furopyrimidines As Phosphoinositide 3-Kinase Inhibitors And Their Pharmaceutical Compositions
    参考文献:World Intellectual Property Organization]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Methanol,Water; 2 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 3
    标题:Five-And-Six-Membered Heterocyclic Compound,Its Preparation Method And Pharmaceutical Application
    参考文献:World Intellectual Property Organization]

    1093066-63-7 = 956034-06-3
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Water; 1.5 H,Reflux1.2 Reagents: Hydrochloric Acid Solvents: Water; Ph 4 - 5
    标题:Preparation Of Heterocyclic Compounds As Janus Kinase Inhibitors
    参考文献:World Intellectual Property Organization
📜3-脲啶呋喃-2-羧酸甲酯置于potassium Tert-Butylate体系中,用 四氢呋喃 作为反应溶剂,化学反应 3.5H,以93.1%的收率获得产物2,4-二羟基呋喃并[3,2-D]嘧啶
参考文献:发现新型和有效的parp / Pi3K双重抑制剂来治疗癌症
标题:发现新型和有效的parp / Pi3K双重抑制剂来治疗癌症
摘要:Parp抑制剂在具有brca突变的癌症中取得了巨大的成功,但是只有一小部分患者携带brca突变,这导致其适应症范围狭窄.最近,越来越多的证据表明,Parp和pi3K抑制剂的组合可能在各种癌症中引起意想不到的协同作用,甚至包括brca熟练的癌症.在这项工作中,设计,合成和评估了一系列parp / Pi3K双重抑制剂的生物活性.发现化合物9A和23A对parp-1(9A:Ic 50 = 1.57 Nm,23A:Ic 50 = 0.91 Nm)和pi3Kα(9A:Ic50 = 2.0 Nm,23A:Ic 50 = 1.5 Nm),并显示出对brca缺乏(hct-116,Hcc-1937)和brca充分(sw620,Mda-Mb-231 / 468)肿瘤细胞的有希望的抗增殖活性.图9A和23A在mda-Mb-468异种移植小鼠模型中也表现出相当大的体内抗肿瘤功效,Tgi值分别为56.39%和48
DOI:10.1016/j.Ejmech.2021.113357

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专利信息


专利号:US-4703120-A
优先权日:1986-04-28
标 题 :Furo(3,4-d)pyrimidine-2,4-dione derivatives and intermediates thereof
发明人：PRESS JEFFERY B
权利人:ORTHO PHARMA CORP
摘要:The synthesis of furo[3,4-d]pyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and furo[3,4-d]pyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.

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合成方法参考DOI号:10.1016/j.ejmech.2021.113357
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