CAS: 852227-95-3; 4-[3-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Phenyl]Morpholine

该化合物其明确界定的结构和与的兼容性使其对制药和材料科学应用具有价值.该产品的特点在于要求高的合成工作流程保持纯度和可靠性能.建议在惰性条件下适当储存在惰性条件下保持其随时间变化.

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran bis(pinacol)diborane 1-(3-bromophenyl)-morpholine 1,1'-oxybis(2-bromo-ethane) {5-methyl-4-[5-(3-morpholin-4-yl-phenyl)-thiophen-2-yl]-pyrimidin-2-yl}-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine 4-(3-(2-chloropyrimidin-4-yl)phenyl)morpholine 8-(3-morpholinophenyl)quinoline-2-carboxylic acid 3-chloro-N-[6-methyl-3-[3-(4-morpholinyl)phenyl]-2-(1H-pyrazol-4-yl)thieno[2,3-b]pyridin-4-yl]benzenesulfonamide

合成工艺路线路线简述

  • 73183-34-3 = 852227-95-3
    反应条件:1.1 Reagents: Lithium Tert-Butoxide Catalysts: Bis(Acetylacetonato)Nickel,1H-Imidazolium,1,3-Bis[2,6-Bis(1-Methylethyl)Phenyl]-4,5-Dimethyl-,Chloride (1... Solvents: Cyclopentyl Methyl Ether; 16 H,100 °C
    标题:Nickel-Catalyzed Ipso-Borylation Of Silyloxyarenes Via C-O Bond Activation
    作者:Pein,Wesley L.; Wiensch,Eric M.; Montgomery,John
    参考文献:Chemrxiv 日期:2021 卷标:1 页码:1-6]

    73183-34-3 + 197846-82-5 = 852227-95-3
    反应条件:1.1 Reagents: Potassium Acetate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,4-Dioxane; 12 H,80 °C
    标题:Kinase Scaffold Repurposing For Neglected Disease Drug Discovery: Discovery Of An Efficacious,Lapatanib-Derived Lead Compound For Trypanosomiasis
    作者:Patel,Gautam; Karver,Caitlin E.; Behera,Ranjan; Guyett,Paul J.; Sullenberger,Catherine; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2013 卷标:56(10) 页码:3820-3832]

    73183-34-3 + 197846-82-5 = 852227-95-3
    反应条件:1.1 Reagents: Potassium Acetate Catalysts: Dichloro[1,1′-Bis(Diphenylphosphino)Ferrocene]Palladium(Ii) Dichloromethane Addu... Solvents: 1,4-Dioxane; 6 H,Rt -> 80 °C
    标题:Protozoan Parasite Growth Inhibitors Discovered By Cross-Screening Yield Potent Scaffolds For Lead Discovery
    作者:Devine,William; Woodring,Jennifer L.; Swaminathan,Uma; Amata,Emanuele; Patel,Gautam; Et Al
    参考文献:Journal Of Medicinal Chemistry 日期:2015 卷标:58(14) 页码:5522-5537]

    73183-34-3 = 852227-95-3
    反应条件:1.1 Reagents: Lithium Tert-Butoxide Catalysts: Bis(Acetylacetonato)Nickel,1H-Imidazolium,1,3-Bis[2,6-Bis(1-Methylethyl)Phenyl]-4,5-Dimethyl-,Chloride (1... Solvents: Cyclopentyl Methyl Ether; 16 H,100 °C
    标题:Nickel-Catalyzed Ipso-Borylation Of Silyloxyarenes Via C-O Bond Activation
    作者:Pein,Wesley L.; Wiensch,Eric M.; Montgomery,John
    参考文献:Organic Letters 日期:2021 卷标:23(12) 页码:4588-4592
📜1,3-二溴苯置于tris-(Dibenzylideneacetone)Dipalladium(0),1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,Potassium Tert-Butylate,Potassium Acetate,4,5-双二苯基膦-9,9-二甲基氧杂蒽体系中,用 1,4-二氧六环,甲苯 作为反应溶剂,化学反应 6.0H,反应生成 3-码啉苯硼酸四甲基二酯
参考文献:Protozoan Parasite Growth Inhibitors Discovered By Cross-Screening Yield Potent Scaffolds For Lead Discovery
标题:Protozoan Parasite Growth Inhibitors Discovered By Cross-Screening Yield Potent Scaffolds For Lead Discovery
摘要:Tropical Protozoal Infections Are A Significant Cause Of Morbidity And Mortality Worldwide; Four In Particular (Human African Trypanosomiasis (Hat),Chagas Disease,Cutaneous Leishmaniasis,And Malaria) Have An Estimated Combined Burden Of Over 87 Million Disability-Adjusted Life Years. New Drugs Are Needed For Each Of These Diseases,Building On The Previous Identification Of Neu-617 (1) As A Potent And Nontoxic Inhibitor Of Proliferation For The Hat Pathogen (Trypanosoma Brucei),We Have Now Tested This Class Of Analogs Against Other Protozoal Species: T. Cruzi (Chagas Disease),Leishmania Major (Cutaneous Leishmaniasis),And Plasmodium Falciparum (Malaria). Based On Hits Identified In This Screening Campaign,We Describe The Preparation Of Several Replacements For The Quinazoline Scaffold And Report These Inhibitors' Biological Activities Against These Parasites. In Doing This,We Have Identified Several Potent Proliferation Inhibitors For Each Pathogen,Such As 4-(3-Chloro-4-((3-Fluorobenzyl)Oxy)Phenyl)Amino)-6-(4-((4-Methyl-1,4-Diazepan-1-yl)Sulfonyl)Phenyl)Quinoline-3-Carbonitrile (Neu-924,83) For T. Cruzi And N-(3-Chloro-4-((3-Fluorobenzypoxy)Phenyl)-7-(4-((4-Methyl-1,4-Diazepan-1-yl)Sulfonyl)Phenyl)Cinnolin-4-Amine (Neu-1017,68) For L. Major And P. Falciparum.
DOI:10.1021/acs.Jmedchem.5B00515

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✅ COA系统入驻 | 共享模式

合成参考文献

参考DOI号:10.1021/acs.jmedchem.5b00515
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