📜(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
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.
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
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