CAS: 86386-76-7; 1-((2-(2,4-Difluorophenyl)Oxiran-2-yl)Methyl)-1H-1,2,4-Triazole

该化合物是一种基于三甲苯的环氧化合物,其基是二氟苯基替代物,可增强其在合成应用中的再活动性和稳定性.环氧和三氮基功能组的存在使其在制药和农用化学合成中具有多种用途的中间体,特别是用于构建异环化框架.其结构僵化性和电排氟基原子有助于改善代谢稳定性和将目标分子的亲近性捆绑在一起.该化合物由于三亚硝基苯基生物活性已知,在开发抗烟和抗微生物剂方面特别宝贵.高纯度和定义明确的立体化学确保研究和工业应用中的再生性.

结构式图片

上下游产品

CAS号1774-47-6 三甲基碘化亚砜 | CAS号86404-63-9 2,4-二氟-α-(1H-1,... | CAS号2181-42-2 三甲基碘代磺酸 | CAS号51336-94-8 2-氯-2,4-二氟苯乙酮 | CAS号372-18-9 1,3-二氟苯 | CAS号70775-39-2 2-(4-chloro-phe... | CAS号86386-73-4 氟康唑 | CAS号118689-07-9 2-(2,4-二氟苯基)-3-...

合成工艺路线路线简述

  • 86386-76-7 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 1 H,0 °C
    标题:Molecular Docking,Design,Synthesis And Antifungal Activity Study Of Novel Triazole Derivatives Containing The 1,2,3-Triazole Group
    作者:Yu,Shichong; Et Al
    参考文献:Rsc Advances 日期:2013 卷标:3(32) 页码:13486-13490]

    86386-76-7 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 1 H,0 °C
    标题:Synthesis And Antifungal Activity Of The Novel Triazole Compounds
    作者:Yu,Shichong; Et Al
    参考文献:Medchemcomm 日期:2013 卷标:4(4) 页码:704-708]

    86386-76-7 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Methanesulfonic Acid; 1 H,0 °C
    标题:Design,Synthesis,And Biological Evaluation Of Novel 1-(1H-1,2,4-Triazole-1-Yl)-2-(2,4-Difluorophenyl)-3-Substituted Benzylamino-2-Propanols
    作者:Chai,Xiaoyun; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2009 卷标:19(6) 页码:1811-1814]

    1774-47-6 + 86404-63-9 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Potassium Hydroxide Solvents: Water; Rt1.2 Solvents: 1,2-Dichloroethane; Rt1.3 Catalysts: Cetrimide; 5 H,Rt1.4 Solvents: Ethyl Acetate; Rt -> 10 °C1.5 Solvents: Ethyl Acetate; 1 H,10 °C
    标题:Process For Preparing 2-(2,4-Difluoro-Phenyl)-1-(1H-1,2,4-Triazole-1-Yl)-2,3-Epoxy-Propane
    参考文献:Hungary]

    1774-47-6 + 86404-63-9 = 86386-76-7 + 75-75-2
    反应条件:1.1 Solvents: Toluene; 3 H,80 °C
    标题:Design,Synthesis,And Antifungal Activities Of Novel 1H-Triazole Derivatives Based On The Structure Of The Active Site Of Fungal Lanosterol 14α-Demethylase (Cyp51)
    作者:Zhao,Qing-Jie; Et Al
    参考文献:Chemistry & Biodiversity 日期:2007 卷标:4(7) 页码:1472-1479]

    1774-47-6 + 86404-63-9 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Toluene; 3 H,60 °C
    标题:Design,Synthesis And Antifungal Activity Of Novel Triazole Derivatives Containing Substituted 1,2,3-Triazole-Piperidine Side Chains
    作者:Jiang,Zhigan; Et Al
    参考文献:European Journal Of Medicinal Chemistry 日期:2014 卷标:82 页码:490-497]

    1774-47-6 + 86404-63-9 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Toluene; 3 H,60 °C
    标题:From Antidiabetic To Antifungal: Discovery Of Highly Potent Triazole-Thiazolidinedione Hybrids As Novel Antifungal Agents
    作者:Wu,Shanchao; Et Al
    参考文献:Chemmedchem 日期:2014 卷标:9(12) 页码:2639-2646]

    1774-47-6 + 51336-94-8 + 288-88-0 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Potassium Carbonate1.2 Reagents: Sodium Hydroxide1.3 -
    标题:Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazole-1-Yl)-2-(2,4-Difluorophenyl)-3-(N-Cyclopropyl-N-Benzyl-Amino)-2-Propanols
    作者:Wu,Wei-Feng; Et Al
    参考文献:Yaoxue Shijian Zazhi 日期:2009 卷标:27(4) 页码:266-269]

    1774-47-6 + 51336-94-8 + 288-88-0 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Potassium Carbonate1.2 Reagents: Dimethyl Sulfoxide
    标题:Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazol-1-Yl)-2-(2,4-Difluorophenyl)-3-(4-Substituted Acyl Piperazin-1-Yl)-2-Propanols
    作者:Liang,Shuang; Et Al
    参考文献:Journal Of Medical Colleges Of Pla 日期:2004 卷标:19(3) 页码:142-145]

    1774-47-6 + 86386-75-6 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Catalysts: Cetrimide Solvents: Toluene; Rt1.2 Reagents: Sodium Hydroxide Solvents: Water; Rt -> 60 °C; 3 H,60 °C; 60 °C -> Rt1.3 Solvents: Ethyl Acetate; Rt -> 0 °C1.4 Solvents: Ethyl Acetate; 1 H,0 °C
    标题:Process For Preparing 2-(2,4-Difluoro-Phenyl)-1-(1H-1,2,4-Triazole-1-Yl)-2,3-Epoxy-Propane
    参考文献:Hungary]

    1774-47-6 + 364-83-0 = 86386-76-7 + 75-75-2
    反应条件:1.1 Solvents: Toluene
    标题:Synthesis And Antifungal Activity Of New Hybrids Thiazolo[4,5-D]Pyrimidines With (1H-1,2,4)Triazole
    作者:Blokhina,Svetlana V.; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2021 卷标:40]

    79-04-9 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Aluminum Chloride2.1 Reagents: Potassium Carbonate2.2 Reagents: Sodium Hydroxide2.3 -
    标题:Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazole-1-Yl)-2-(2,4-Difluorophenyl)-3-(N-Cyclopropyl-N-Benzyl-Amino)-2-Propanols
    作者:Wu,Wei-Feng; Et Al
    参考文献:Yaoxue Shijian Zazhi 日期:2009 卷标:27(4) 页码:266-269]

    = 86386-76-7 + 75-75-2
    反应条件:1.1 Catalysts: Aluminum Chloride; 5 H,50 °C2.1 Reagents: Sodium Bicarbonate Solvents: Toluene; 5 H,Reflux3.1 Reagents: Sodium Hydroxide Catalysts: Hexadecyltrimethylammonium Bromide Solvents: Toluene; 3 H,60 °C3.2 1 H,0 °C
    标题:Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazole-1-Yl)-2-(2,4-Difluorophenyl)-3-Substituted-2-Propanol
    作者:Zhou,Yu; Et Al
    参考文献:Dier Junyi Daxue Xuebao 日期:2011 卷标:32(7) 页码:754-758]

    86386-76-7 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 1 H,0 °C
    标题:Synthesis And Antifungal Activity Of The Novel Triazole Derivatives Containing 1,2,3-Triazole Fragment
    作者:Yu,Shichong; Et Al
    参考文献:Archives Of Pharmacal Research 日期:2013 卷标:36(10) 页码:1215-1222]

    1774-47-6 + 51336-94-8 + 288-88-0 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Sodium Bicarbonate,Potassium Carbonate
    标题:Synthesis And Antifungal Activity Of 1-(1H-1,2,4-Triazol-1-Yl)-2-(2,4-Difluorophenyl)-3-[(4-Substituted)-1-Piperazinyl]-2-Propanols
    作者:Liang,Shuang; Et Al
    参考文献:Zhongguo Yaowu Huaxue Zazhi 日期:2004 卷标:14(2) 页码:71-75]

    1774-47-6 + 86386-75-6 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Sodium Hydroxide,Cetrimide Solvents: Toluene,Water; 3 H,60 °C1.2 Reagents: Methanesulfonic Acid Solvents: Ethyl Acetate; 1 H,0 °C
    标题:Rapid Synthesis Of Some New Propanol Derivatives Analogous To Fluconazole Under Microwave Irradiation In A Solventless System
    作者:Heravi,Majid M.; Et Al
    参考文献:Heterocyclic Communications 日期:2005 卷标:11(1) 页码:19-22]

    1774-47-6 + 79-04-9 + 288-88-0 + 75-75-2 = 86386-76-7 + 75-75-2
    反应条件:1.1 Catalysts: Aluminum Chloride1.2 Reagents: Sodium Bicarbonate1.3 -1.4 -
    标题:Synthesis And Antifungal Activity Of Triazole Derivatives
    作者:Hu,Xiaoyan; Et Al
    参考文献:Huaxue Yanjiu Yu Yingyong 日期:2010 卷标:22(12) 页码:1573-1577]

    86404-63-9 + 75-75-2 + 1030268-24-6 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Toluene; 4 H,60 °C1.2 1.5 H,0 °C
    标题:Synthesis And Antifungal Activities Of Novel Triazole Derivatives With Dithiocarbamates Side Chain
    作者:Zhang,Zhiqiang; Et Al
    参考文献:Yaoxue Fuwu Yu Yanjiu 日期:2016 卷标:16(2) 页码:94-97]

    154534-83-5 = 86386-76-7 + 75-75-2
    反应条件:1.1 Solvents: Water; Rt -> 0 °C1.2 Reagents: Hydrochloric Acid Solvents: Water; 0 - 5 °C1.3 Reagents: Sodium Nitrite Solvents: Water; 0 - 5 °C1.4 Solvents: Dichloromethane1.5 Reagents: Ammonium Hydroxide Solvents: Water; Ph 102.1 Reagents: Sodium Hydroxide Catalysts: Hexadecyltrimethylammonium Bromide Solvents: Water; 3 H,60 °C; 60 °C -> Rt2.2 Solvents: Ethanol; Rt -> 0 °C2.3 Solvents: Acetonitrile; 0 - 5 °C
    标题:Process For Producing 1-[2-(2,4-Difluorophenyl)-2,3-Epoxypropyl]-1H-1,2,4-Triazole And Its Salts
    参考文献:Hungary]

    51336-94-8 + 288-88-0 = 86386-76-7 + 75-75-2
    反应条件:1.1 Reagents: Benzyltriethylammonium Chloride,Potassium Carbonate Solvents: Dichloromethane; 15 - 20 H,0 °C -> Rt2.1 Reagents: Hexadecyltrimethylammonium Bromide,Sodium Hydroxide Solvents: Toluene; 3 - 5 H,60 °C2.2 Solvents: Ethyl Acetate
    标题:Novel Triazoles With Potent And Broad-Spectrum Antifungal Activity In-Vitro And In-Vivo
    作者:Zhu,Panhu; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2023 卷标:66(11) 页码:7497-7515]

    51336-94-8 + 584-13-4 = 86386-76-7 + 75-75-2
    反应条件:1.1 Solvents: Isopropanol; 12 H,Rt2.1 Solvents: Water; Rt -> 0 °C2.2 Reagents: Hydrochloric Acid Solvents: Water; 0 - 5 °C2.3 Reagents: Sodium Nitrite Solvents: Water; 0 - 5 °C2.4 Solvents: Dichloromethane2.5 Reagents: Ammonium Hydroxide Solvents: Water; Ph 103.1 Reagents: Sodium Hydroxide Catalysts: Hexadecyltrimethylammonium Bromide Solvents: Water; 3 H,60 °C; 60 °C -> Rt3.2 Solvents: Ethanol; Rt -> 0 °C3.3 Solvents: Acetonitrile; 0 - 5 °C
    标题:Process For Producing 1-[2-(2,4-Difluorophenyl)-2,3-Epoxypropyl]-1H-1,2,4-Triazole And Its Salts
    参考文献:Hungary
📜1,3-二氟苯置于aluminum (Iii) Chloride,三甲基碘化亚砜,十六烷基三甲基溴化铵,碳酸氢钠,Sodium Hydroxide体系中,用 甲苯 作为反应溶剂,化学反应 13.0H,反应生成 1-[2-(2,4-二氟苯基)-2,3-环氧基丙基]-1H-1,2,4-噻唑
参考文献:Design,Synthesis,And Biological Evaluation Of Novel 1,2,4-Triazole Derivatives As Antifungal Agent
标题:Design,Synthesis,And Biological Evaluation Of Novel 1,2,4-Triazole Derivatives As Antifungal Agent
摘要:设计并合成了一系列新型1,2,4-三氮唑衍生物(9A-p),这些化合物被作为潜在的抗真菌剂.所有化合物均通过1H-NMR,13C-NMR和lcms进行了表征.通过测定最小抑制浓度,评估了它们对七种人类病原性真菌的体外抗真菌活性.发现大多数测试化合物对白色念珠菌的活性强于对照药物氟康唑.
DOI:10.1007/s12272-012-1105-8

海关参考信息

专利信息


专利号:RU-2039050-C1
优先权日:1989-09-26
标 题:Derivatives of 1,2,4-triazole, optically inert or containing r- or s-configuration at c-2 and c-3 asymmetric centers, or their salts showing fungicide activity, and a method of their synthesis

专利号:CN-113354625-B
优先权日:2021-06-16
标 题:Synthesis process of voriconazole

专利号:CN-113354625-A
优先权日:2021-06-16
标题:The synthesis process of voriconazole

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✅ COA系统入驻 | 共享模式

合成参考文献


摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 468.
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