CAS: 483-18-1; (2S,3R,11Bs)-2-(((R)-6,7-Dimethoxy-1,2,3,4-Tetrahydroisoquinolin-1-yl)Methyl)-3-Ethyl-9,10-Dimethoxy-1,3,4,6,7,11B-Hexahydro-2H-Pyrido[2,1-A]Isoquinoline

该化合物是一种自然产生的藻类,产自Cephaelis ipecatuanha(通称为异丙酸)植物,其特点是结构复杂,包括四环框架,其特点是结构复杂,包括四环框架,该化合物展示了各种生物活动,主要因其乳酸性能而得到承认,引起呕吐. (-)-美食作为抗亚moebic剂,使其有效防治某些寄生虫感染,特别是Entamoeba 心肺炎引起的嗜血性痢疾.禁止目标细胞蛋白合成的物质功能导致细胞死亡.除了其药用用途外,(-)-美食还研究其潜在的抗癌特性,因为它可在不同癌症细胞线上诱发骨缩.然而,其使用仅限于潜在的毒性和副作用,包括胃肠扰动和心脏并发症.作为受管制的物质,(-)-美食受许多国家的管制物质受管制,其治疗用途受到仔细监测,其治疗应用导致细胞死亡.

结构式图片

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CAS号1609-47-8 焦碳酸二乙酯 | CAS号105-58-8 碳酸二乙酯 | CAS号90-05-1 愈创木酚 | CAS号75-50-3 三甲胺 | CAS号577-68-4 4,5-二甲氧基邻苯二甲酸

合成工艺路线路线简述

    📜(S)-Tert-Butyl 1-Allyl-6,7-Dimethoxy-3,4-Dihydroisoquinoline-2(1H)-Carboxylate置于rucl2(1,3-Dimesityl-Imidazolidin-2-yl)(Pcy3)(=chph),Palladium On Activated Charcoal,Cl[(1S,2S)-N-P-Ts-1,2-Diphenylethanediamine](P-Cymene)Ru(II) 甲酸,三氟甲磺酸三甲基硅酯,氢气,三甲基铝,苯基锂,三乙胺,三氯氧磷体系中,用 四氢呋喃,甲醇,正己烷,二氯甲烷,N,N-二甲基甲酰胺,苯 作为反应溶剂,化学反应 49.1H,反应生成 依米丁
    参考文献:Formal Total Synthesis Of (−)-Emetine Using Catalytic Asymmetric Allylation Of Cyclic Imines As A Key Step
    标题:Formal Total Synthesis Of (−)-Emetine Using Catalytic Asymmetric Allylation Of Cyclic Imines As A Key Step
    摘要:Catalytic Asymmetric Allylation Of 3,4-Dihydro-6,7-Dimethoxyisoquinoline Was Carried Out Using Allyltrimethoxysilane In The Presence Of Cu(I) And Tol-Binap. The Allyl Adduct Thus Obtained Was Transformed To A Chiral Synthetic Intermediate For (-)-Emetine In Good Yield. The Procedure Was Applied To The Total Synthesis Of Ent-Emetine.
    DOI:10.1021/ol0530326

    海关参考信息

    专利信息


    专利号:US-9409879-B2
    优先权日:2011-03-29
    标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
    发明人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
    权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
    摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

    专利号:US-2014378538-A1
    优先权日:2011-12-14
    标 题:Methods of responding to a biothreat
    发明人:BANCEL STEPHANE
    权利人:MODERMA THERAPEUTICS INC
    摘要:The present disclosure provides for devices, in particular mobile devices, which may be used in the synthesis of modified nucleic acid molecules, in particular modified mRNA molecules. The device for making the modified nucleosides, modified nucleotides and modified nucleic acids (e.g., mRNA) disclosed herein may be mobile devices comprising at least one sample block for insertion of one or more sample vessels, a device base with electronic control units for the sample block, a voltage supply, and one or more reagent(s) for the synthesis of at least one nucleic acid.

    专利号:US-11649285-B2
    优先权日:2016-08-03
    标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
    发明人:KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
    权利人:BIO TECHNE CORP
    摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

    专利号:US-2023212216-A1
    优先权日:2019-12-20
    标 题:Synthesis of lactone derivatives and their use in the modification of proteins
    发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH
    权利人:GENIE BIOTECH UK LTD
    摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.

    专利号:US-2008267981-A1
    优先权日:2004-06-30
    标题:Compositions and Methods for Delivery of Antitumor Agents
    发明人:JANDA KIM D; WIRSCHING PETER; BOGER DALE L
    权利人:SCRIPPS RESEARCH INST
    摘要:Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.

    专利号:US-2025289827-A1
    优先权日:2022-12-02
    标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
    发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
    权利人:C4 THERAPEUTICS INC
    摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

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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


    1: Bleasel MD, Peterson GM. Emetine, Ipecac, Ipecac Alkaloids and Analogues as Potential Antiviral Agents for Coronaviruses. Pharmaceuticals (Basel). 2020 Mar 21;13(3):E51. doi: 10.3390/ph13030051. 20(23):5914. doi: 10.3390/ijms20235914.
    3: Tang Q, Li S, Du L, Chen S, Gao J, Cai Y, Xu Z, Zhao Z, Lan K, Wu S. Emetine protects mice from enterovirus infection by inhibiting viral translation. Antiviral Res. 2020 Jan;173:104650. doi: 10.1016/j.antiviral.2019.104650. Epub 2019 Nov 14. 11(10):964. doi: 10.3390/v11100964.
    6: Siddique MAH, Satoh K, Kurosawa R, Kikuchi N, Elias-Al-Mamun M, Omura J, Satoh T, Nogi M, Sunamura S, Miyata S, Ueda H, Tokuyama H, Shimokawa H. Identification of Emetine as a Therapeutic Agent for Pulmonary Arterial Hypertension: Novel Effects of an Old Drug. Arterioscler Thromb Vasc Biol. 2019 Nov;39(11):2367-2385. doi: 10.1161/ATVBAHA.119.313309. Epub 2019 Sep 19. 42(5):1735-1744. doi: 10.3892/or.2019.7290. Epub 2019 Aug 22.

    合成参考文献


    参考文献:10.1113/jphysiol.2011.209379
    摘要:Connor SA, Wang YT, Nguyen PV. Activation of β‐adrenergic receptors facilitates heterosynaptic translation‐dependent long‐term potentiation. The Journal of Physiology. 2011 Aug 30;589(17):4321–40. doi: 10.1113/jphysiol.2011.209379.
    参考文献:10.3390/ijms12064027
    摘要:Prussia A, Thepchatri P, Snyder JP, Plemper RK. Systematic approaches towards the development of host-directed antiviral therapeutics. Int J Mol Sci. 2011;12(6):4027–52.
    参考文献:10.1371/journal.pone.0021568
    摘要:Mei F, Nagappan G, Ke Y, Sacktor TC, Lu B. BDNF Facilitates L-LTP Maintenance in the Absence of Protein Synthesis through PKMζ. PLoS ONE. 2011 Jun 29;6(6):e21568. doi: 10.1371/journal.pone.0021568.
    参考文献:10.1371/journal.pone.0021585
    摘要:Dredge BK, Jensen KB. NeuN/Rbfox3 Nuclear and Cytoplasmic Isoforms Differentially Regulate Alternative Splicing and Nonsense-Mediated Decay of Rbfox2. PLoS ONE. 2011 Jun 29;6(6):e21585. doi: 10.1371/journal.pone.0021585.
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