CAS: 21617-12-9; 4,8-Dichloroquinoline

该化合物是一种卤化的奎宁衍生物,在制药和农用化学研究中具有显著应用性,其结构以4和8个位置的氯替代物为特色,增强了反应性,并充当综合生物活性化合物的多功能中间体,该化合物因其作为更复杂的循环系统前体的能力而在抗微生物剂和抗疟剂的开发中的作用而特别受到重视,在标准条件下保持稳定,与各种合成途径相兼容,因此成为实验和工业用途的实际选择,二氯化框架还促进进一步发挥作用,扩大其在医药化学中的用途.

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合成工艺路线路线简述

    📜5-[(2-Chloro-Phenylamino)-Methylene]-2,2-Dimethyl-[1,3]Dioxane-4,6-Dione置于三氯氧磷体系中,用 二苯醚 用作溶剂,化学反应 3.08H,反应生成4,8-二氯喹啉
    参考文献:Synthesis Of Ring-Substituted 4-Aminoquinolines And Evaluation Of Their Antimalarial Activities
    标题:Synthesis Of Ring-Substituted 4-Aminoquinolines And Evaluation Of Their Antimalarial Activities
    摘要:A Simple Two-Step Synthesis Method Was Used To Make 51 B-Ring-Substituted 4-Hydroxyquinolines Allowing Analysis Of The Effect Of Ring Substitutions On Inhibition Of Growth Of Chloroquine Sensitive And Resistant Strains Of Plasmodium Falciparum,The Dominant Cause Of Malaria Morbidity. Substituted Quinoline Rings Other Than The 7-Chloroquinoline Ring Found In Chloroquine Were Found To Have Significant Activity Against The Drug-Resistant Strain Of P. Falciparum W2. (C) 2004 Elsevier Ltd. All Rights Reserved.
    Doi:10.1016/j.Bmcl.2004.12.037

    海关参考信息

    专利信息


    专利号:US-2007060558-A1
    优先权日:2004-07-30
    标 题 :Hybrid molecules QA where Q is an aminoquinoline and A is an antibiotic residue, the synthesis and uses thereof as antibacterial agents
    发明人:SANCHEZ MURIEL; MEUNIER BERNARD
    权利人:CENTRE NAT RECH SCIENT
    摘要:The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q—(Y 1 ) p —(U) p —(Y 2 ) p -A: wherein Q represents an aminoquinoline, (Y 1 ) p (U) p —(Y 2 ) p″ is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献

    参考标题:Antimalarials: Synthesis Of 4-Aminoquinolines That Circumvent Drug Resistance In Malaria Parasites
    作者:Dibyendu De,Larry D. Byers,Donald J. Krogstad |发布日期:1997.1
    摘要:Substitution With Neat Amine Rather Than In Phenol, Regioselective Reductive Alkylation To Convert The Terminal Primary Amine (12A-20A) On The Diaminoalkane Side Chain To A Diethylamino Group, And Purification By Column Chromatography With Basic Alumina. The 1H Nmr Spectra Obtained After Regioselective Reductive Alkylation With Sodium Borodeuteride (In Comparison With Sodium Borohydride) Demonstrated That

    合成参考文献


    摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 145.
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