CAS: 136816-75-6; (4-(3-(Ethylamino)Pyridin-2-yl)Piperazin-1-yl)(5-Methoxy-1H-Indol-2-yl)Methanone

该化合物是一种合成化合物,被归类为非核反转转转录酶抑制剂(NNRTI),主要用于治疗艾滋病毒感染,有选择地抑制反转发录酶酶,这对艾滋病毒的复制至关重要,阿提弗丁展示了独特的化学结构,使其能与酶结合,从而防止病毒性RNA转化为DNA,这是病毒性生命周期中的一个关键步骤;该化合物的特点是其中性亲口性,影响其吸收和在体内的分布;阿特维迪因在临床实践中虽然与其他抗逆转录病毒剂相比没有被广泛使用,但其效力和安全性却得到了研究;其药性活性,包括新陈代谢和排泄物,对于了解其治疗潜力和与其他药物的相互作用十分重要;总体而言,阿特维尔丁是当前努力发展有效艾滋病毒/艾滋病治疗的一个重要研究领域.

结构式图片

合成工艺路线路线简述

    📜在 1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,Sodium Hydroxide体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 18.0H,反应生成阿替韦啶
    参考文献:钴催化分子内酰胺化通过氧化诱导还原消除途径合成吲哚
    标题:钴催化分子内酰胺化通过氧化诱导还原消除途径合成吲哚
    摘要:使用高价钴催化的 C-H 键活化和功能化通常涉及 Co(III)/co(I) 催化循环.由于缺乏与 Co(Iv) 中间体的高反应性和不稳定性相关的证据和挑战,涉及 Co(Iv) 中间体的 C-H 官能化机制研究的报告仍未得到充分探索.在此,我们报道了通过 α-酰胺丙烯酸酯的分子内酰胺化有效合成吲哚-2-羧酸酯,并对反应机理进行了实验和计算研究,其中涉及 Co(Iv) 物质的氧化诱导还原消除.
    Doi:10.1021/acscatal.3C05706

    海关参考信息

    专利信息


    专利号:US-2006115536-A1
    优先权日:2004-11-12
    标 题 :Glycerin based synthesis of silver nanoparticles and nanowires
    发明人:YACAMAN MIGUEL J; ELECHIGUERRA JOSE L; BURT JUSTIN L; MORONES JOSE R; LOPEZ LETICIA L
    权利人:UNIV TEXAS
    摘要:The present invention includes compositions and methods for the production of noble metal nanoparticles and nanowires conjugated to polyols or polymers. The present invention allows the incorporation of noble metal nanoparticles to a wide range of products such as body care products to exploit the biocidal properties of silver nanoparticles against bacteria, viruses and fungi.

    专利号:WO-2007001453-A9
    优先权日:2004-11-15
    标 题:Glycerin based synthesis of silver nanoparticles and nanowires
    发明人:YACAMAN MIGUEL JOSE; ELECHIGUERRA JOSE LUIS; BURT JUSTIN LOCKHEART; MORONES JOSE RUBEN; LARIOS LETICIA
    权利人:UNIV TEXAS; YACAMAN MIGUEL JOSE; ELECHIGUERRA JOSE LUIS; BURT JUSTIN LOCKHEART; MORONES JOSE RUBEN; LARIOS LETICIA
    摘要:The present invention includes compositions and methods for the production of noble metal nanoparticles and nanowires conjugated to polyols or polymers. The present invention allows the incorporation of noble metal nanoparticles to a wide range of products such as body care products to exploit the biocidal properties of silver nanoparticles against bacteria, viruses and fungi.

    专利号:US-11472706-B2
    优先权日:2017-11-30
    标 题:Hydroxyapatite composite for use in removal of contaminants from effluents and methods of making
    发明人:DELPLANCHE THIERRY; MIMOUNI AZIZ; LE MERCIER THIERRY; KHIRANI SARAH; D'ALENCON LAURIANE; ANTOINETTE YVES; ORTEGO BEATRICE
    权利人:SOLVAY
    摘要:A composite comprising a hydroxyapatite and at least one additive which is present during hydroxyapatite synthesis. The additive may be embedded or incorporated into or coated onto the hydroxyapatite. The additive preferably increases the hydroxyapatite porosity, e.g., providing a higher pore volume and/or BET surface area than a hydroxyapatite material without additive. The additive preferably comprises an activated carbon, chitosan, hopcalite, clays, zeolites, sulfur, and/or a metal such as Al, Sn, Ti, Fe, Cu, Zn, Ni, Cu, Zr, La, Ce, in the form of metal, salt, oxide, oxyhydroxide, and/or hydroxide. The hydroxyapatite may be calcium-deficient. The composite is in the form of particles having a D50 of at least 20 μm, a BET surface area of at least 120 m2/g; and/or a total pore volume of at least 0.3 cm3/g. An adsorbent material comprising a composite or a blend of composite with a hydroxyapatite without additive, and its use for removal of contaminants such as Hg, Se, As, and/or B from an effluent.

    专利号:EP-1817042-A2
    优先权日:2004-11-15
    标 题:Glycerin based synthesis of silver nanoparticles and nanowires

    专利号:CA-2587314-A1
    优先权日:2004-11-15
    标题 :Glycerin based synthesis of silver nanoparticles and nanowires

    专利号:WO-2007001453-A2
    优先权日:2004-11-15
    标题:Glycerin based synthesis of silver nanoparticles and nanowires

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Galal SA, Abd El-All AS, Abdallah MM, El-Diwani HI. Synthesis of potent antitumor and antiviral benzofuran derivatives. Bioorg Med Chem Lett. 2009 May 1;19(9):2420-8. doi: 10.1016/j.bmcl.2009.03.069. Epub 2009 Mar 21. 45(1):47-58. doi: 10.1016/s0166-3542(99)00073-x. 19(2):135-44. doi: 10.1097/00042560-199810010-00006. 26(10):1008-18. 39(2):298-302. 40(6):847-53. doi: 10.1093/jac/40.6.847. 693(2):431-6. doi: 10.1016/s0378-4347(97)00090-x. 40(11):2664-8. doi: 10.1128/AAC.40.11.2664.
    9: Brew BJ, Dunbar N, Druett JA, Freund J, Ward P. Pilot study of the efficacy of atevirdine in the treatment of AIDS dementia complex. AIDS. 1996 Oct;10(12):1357-60. doi: 10.1097/00002030-199610000-00007. 39(19):3769-89. doi: 10.1021/jm960158n. 40(3):767-71. doi: 10.1128/AAC.40.3.767.
    12: Been-Tiktak AM, Vrehen HM, Schneider MM, van der Feltz M, Branger T, Ward P, Cox SR, Harry JD, Borleffs JC. Safety, tolerance, and pharmacokinetics of atevirdine mesylate (U-87201E) in asymptomatic human immunodeficiency virus- infected patients. Antimicrob Agents Chemother. 1995 Mar;39(3):602-7. doi: 10.1128/AAC.39.3.602.

    合成参考文献


    参考文献:10.3797/scipharm.1012-17
    摘要:Bielenica A, Kossakowski J, Struga M, Dybała I, Loddo R, Ibba C, La Colla P. Synthesis and Biological Evaluation of New 3-Phenyl-1-[(4-arylpiperazin-1-yl)alkyl]-piperidine-2,6-diones. Sci Pharm. 2011 Apr;79(2):225–38.
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