CAS: 6153-64-6; (4S,4Ar,5S,5Ar,6S,12As)-4-(Dimethylamino)-3,5,6,10,12,12A-Hexahydroxy-6-Methyl-1,11-Dioxo-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide Dihydrate

该化合物是一种四环乙烷主要用于兽医,有时用于人类医学的广义抗生素,主要用于兽医和人类医学,其特点是它能够抑制细菌蛋白合成,与30S 脊髓膜炎亚元素结合,使其对范围广泛的克阳性和克阴性细菌有效,二氢酸盐形式表明,化合物含有两种水分子,可影响其溶性与稳定性.二氢氧化丙烷通常是一种黄色至橙色晶状粉,有轻微的味道;它溶于水中,呈现出一种依赖丙基溶性,酸性更强的蛋白质特征,该化合物对光敏感,应储存在一个冷干的地方以保持其功效.此外,它可能具有副作用,包括气态肠扰动和潜在的过敏反应,其使用受到关于抗生素抗药性的条例的约束.

结构式图片

欧盟法规

C&L通报REACH预注册

合成工艺路线路线简述

    专利信息


    专利号:WO-2012047907-A9
    优先权日:2010-10-04
    标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
    发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
    权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN
    摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.

    专利号:US-9688644-B2
    优先权日:2009-04-30
    标 题 :Synthesis of Tetracyclines and intermediates thereto
    发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M
    权利人:HARVARD COLLEGE
    摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.

    专利号:US-10768157-B2
    优先权日:2015-10-20
    标 题:Materials and methods for the detection of trace amounts of substances in biological and environmental samples
    发明人:KABIR ABUZAR; FURTON KENNETH G
    权利人:KABIR ABUZAR; FURTON KENNETH G; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
    摘要:The subject invention provides chemical compositions and synthesis strategies to create molecularly imprinted polymers (MIPs) via sol-gel processes. In a specific embodiment, the subject invention utilizes a(n) organic, inorganic, or metallic template analyte to create a hybrid organic-inorganic or inorganic three-dimensional network possessing cavities complementary to the shape, size, and functional orientation of the template molecule or ions. The subject invention further pertains to the use of the novel MIPs as selective solid phase extraction (SPE) sorbents for pre-concentration and clean-up of trace substances in biological and environmental samples. Synthesis of other molecularly imprinted polymers with environmental, pharmaceutical, chemical, clinical, toxicological, and national security implications can be conducted in accordance with the teachings of the subject invention.

    专利号:US-9884830-B2
    优先权日:2004-05-21
    标题 :Synthesis of tetracyclines and analogues thereof
    发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R
    权利人:HARVARD COLLEGE
    摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.

    专利号:US-8907104-B2
    优先权日:2006-10-11
    标 题 :Synthesis of enone intermediate
    发明人:MYERS ANDREW G; BRUBAKER JASON D
    权利人:HARVARD COLLEGE
    摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

    专利号:US-10925977-B2
    优先权日:2006-10-05
    标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
    发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
    权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
    摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
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    主要参考文献


    1: Gao C, Liu Z, Chen J, Yan Z. A novel fluorescent assay for oxytetracycline hydrochloride based on fluorescence quenching of water-soluble CdTe nanocrystals. Luminescence. 2013 May-Jun;28(3):378-83. doi: 10.1002/bio.2393. Epub 2012 Jun 19. doi: 10.1111/j.1524-4725.2012.02399.x. Epub 2012 Mar 27. doi: 10.1111/j.1095-8649.2010.02887.x. doi: 10.2460/javma.237.5.555. German. Croatian. Dutch. Croatian. Russian.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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