CAS: 1207283-85-9; (4S,4As,5Ar,12As)-4-(Dimethylamino)-7-Fluoro-3,10,12,12A-Tetrahydroxy-1,11-Dioxo-9-(2-(Pyrrolidin-1-yl)Acetamido)-1,4,4A,5,5A,6,11,12A-Octahydrotetracene-2-Carboxamide

该化合物是一个复杂的有机化合物,其特点是多环形结构和各种功能组.该物质具有环烷基脊柱,有助于其潜在的生物活动.氨基碳基基基质组的存在表明,它可能参与氢联结和其他互动,增强它的溶性与再活性.二甲基氨基质组群表明,它的基本特性可能会影响其药理学和与生物目标的相互作用.此外,氟基质原子可能会进一步增强它的代谢稳定性和脂性.该化合物在多种染基化学中心的具体配置显示的立体化学反应,但这种化学特性应用可能对其具体生物化学制剂的稳定性至关重要.

结构式图片

合成工艺路线路线简述

    📜(4S,4As,5Ar,12As)-9-Amino-4-(Dimethylamino)-7-Fluoro-1,4,4A,5,5A,6,11,12A-octahydro-3,10,12,12A-Tetrahydroxy-1,11-Dioxo-2-Naphthacenecarboxamide Dihydrochloride,2-(Pyrrolidin-1-yl)Acetyl Chloride置于2-(Pyrrolidin-1-yl)Acetyl Chloride体系中,用88.7的收率获得依拉环素
    参考文献:Org. Process Res. Dev. 2013,17,838-845
    标题:Org. Process Res. Dev. 2013,17,838-845

    海关参考信息

    专利信息


    专利号:US-10065924-B2
    优先权日:2014-07-22
    标 题 :Preparation and biological evaluation of viridicatumtoxin analogs
    发明人:NICOLAOU KYRIACOS C; HALE CHRISTOPHER R H; NILEWSKI CHRISTIAN; IOANNIDOU HERAKLIDIA; EL MARROUNI ABDELLATIF
    权利人:UNIV RICE WILLIAM M
    摘要:In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.

    专利号:PT-117254-B
    优先权日:2021-05-26
    标题 :METHOD FOR SYNTHESIS OF 9-AMINOMETHYL TETRACYCLINE COMPOUNDS

    专利号:US-11980627-B2
    优先权日:2019-06-14
    标 题 :Triple pharmaceutical composition for proteinaceous infection
    发明人:ATIBA JOSHUA O
    权利人:ATIBA JOSHUA O
    摘要:There are disclosed therapies and preventions of prion protein complex infections. The transcription of the amyloid precursor protein gene and PrP gene and the RNA transcript are the rate-limiting steps and are most susceptible for blockage and control of the process of amyloid protein formation and PrP sc formation. Thus, therapies and prevention regimes for prion protein complex infections interrupt this process at the level of DNA transcription to RNA, RNA transport to the mitochondrion for protein synthesis and deposition in the cerebral cortex neurons.

    专利号:US-12291515-B2
    优先权日:2021-12-22
    标 题 :Pyrrolidine derivative and use thereof
    发明人:WANG ZHEMING; TAN HAO
    权利人:WANG ZHEMING; RUSHI BIOTECH HANGZHOU CO LTD
    摘要:The present invention discloses a pyrrolidine derivative or its optically active isomer, or a pharmaceutically acceptable salt thereof, which is useful as an NAMPT inhibitor, and useful as a potential agent for the chemotherapy of a variety of diseases associated with abnormal NAD+ expression. The pyrrolidine derivative has pyrrolidine as a parent structure, to which pyridinylurea (or substituted pyridinylurea) is attached by an intermediate aliphatic chain, and a side arylformyl (or heterocyclylformyl) group is attached. This structure is an optimized structure of the NAMPT inhibitor FK866, in which the acrylamido group is replaced by a urea structure, to increases the water solubility of the compound. Moreover, the difficulty in synthesis is reduced accordingly, which is conducive to the subsequent industrial production.

    专利号:US-10501454-B2
    优先权日:2016-07-21
    标 题 :Monocyclic β-lactam-siderophore conjugate, and preparation method and use thereof
    发明人:YANG YUSHE; TAN LIANG; KOU QUNHUAN
    权利人:YANG YUSHE; TAN LIANG; KOU QUNHUAN; SHANGHAI INST MATERIA MEDICA CAS
    摘要:The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic β-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic β-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Jackson MNW, Wei W, Mang NS, Prokesch BC, Ortwine JK. Combination eravacycline therapy for ventilator-associated pneumonia due to carbapenem- resistant Acinetobacter baumannii in patients with COVID-19: A case series. Pharmacotherapy. 2024 Jan 25. doi: 10.1002/phar.2908. Epub ahead of print. 12(1):e0235123. doi: 10.1128/spectrum.02351-23. Epub 2023 Nov 29.
    3: Alexander C, Hill D. A retrospective case-control study of eravacycline for the treatment of carbapenem-resistant Acinetobacter infections in patients with burn injuries. J Burn Care Res. 2023 Nov
    16:irad183. doi: 10.1093/jbcr/irad183. Epub ahead of print. 57(4):608-624. Turkish. doi: 10.5578/mb.20239949. 21(11):1259-1267. doi: 10.1080/14787210.2023.2270160. Epub 2023 Nov 8. 366(6):464-467. doi: 10.1016/j.amjms.2023.09.012. Epub 2023 Sep 15.

    合成参考文献


    参考文献:10.1177/2168479017750129
    摘要:Baldrick P. Juvenile Animal Testing: Assessing Need and Use in the Drug Product Label. Ther Innov Regul Sci. 2018 Sep;52(5):641–8. doi: 10.1177/2168479017750129.
    参考文献:10.1038/s41579-019-0218-1
    摘要:Andersson DI, Nicoloff H, Hjort K. Mechanisms and clinical relevance of bacterial heteroresistance. Nat Rev Microbiol. 2019 Aug;17(8):479–96. doi: 10.1038/s41579-019-0218-1.
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