CAS: 65271-80-9; 1,4-Dihydroxy-5,8-Bis((2-((2-Hydroxyethyl)Amino)Ethyl)Amino)Anthracene-9,10-Dione

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CAS号81-59-4 9,10-Anthracene... | CAS号131401-54-2 1,4-Difluoro-5,... | CAS号111-41-1 羟乙基乙二胺

2,3-二氢-1,4,5,8-四羟基-9,10-蒽醌置于四甲基乙二胺,四氯苯醌体系中,用 乙二醇甲醚 作为反应溶剂,化学反应生成 米托蒽醌
参考文献:Antitumor Agents. 1. 1,4-Bis[(Aminoalkyl)Amino]-9,10-Anthracenediones
标题:Antitumor Agents. 1. 1,4-Bis[(Aminoalkyl)Amino]-9,10-Anthracenediones
摘要:The Condensation Of Alkylenediamines With Quinizarin Or With 2,3-Dihydro-1,4,5,8-Tetrahydroxy-9,10-Anthracenedione,Followed By Oxidation,Gave 1,4-Bis[aminoalkyl)Amino]-9,10-Anthracenediones. Some Of These Compounds And Their 2,3-Dihydro Derivatives Were Markedly Active Against Both Leukemias And Solid Tumors In Mice. Activity Was Maximal With 5,8-Dihydroxylation And 1,4-Bis[(2-Aminoethyl)Amino] Substitution,In Which The Terminal Nitrogen Atoms Were Either Unsubstituted (Compound 50) Or Carried 2-Hydroxyethyl Groups (Compound 40),Indicating The Importance Of Hydrophilicity. Against B-16 Melanoma,50 Gave Greater Than 433% Increase In Median Life Span (Ils) With 7/10 80-Day Survivors. Against P-388 Leukemia,40 Gave Greater Than 500% Ils With 4/5.60-Day Survivors; Its Efficacy And Therapeutic Index Equaled Or Surpassed Those Of Adriamycin,Cyclophosphamide,Daunorubicin,Methotrexate,Or 5-Fluorouracil. Against L-1210 Leukemia,B-16 Melanoma,And Colon Tumor 26,40 Was Generally As Effective Or More Effective Than Adriamycin And Is Now Undergoing Preclinical Toxicological Evaluation.
DOI:10.1021/jm00195A002

专利信息

专利号:US-2004242897-A1
优先权日:2002-07-31
标题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:WO-2004011474-A1
优先权日:2002-07-31
标题:Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-6653468-B1
优先权日:2002-07-31
标 题 :Universal support media for synthesis of oligomeric compounds
发明人：GUZAEV ANDREI P; MANOHARAN MUTHIAH
权利人:ISIS PHARMACEUTICALS INC
摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.

专利号:US-3983145-A
优先权日:1973-11-01
标 题:Use of alpha-di(lower alkoxy) anthraquinones in the synthesis of Alizarin Saphirols
发明人：WHITE DAVID L; FITZPATRICK JOSEPH W
权利人:TOMS RIVER CHEMICAL CORP
摘要:Alpha-dihydroxyanthraquinones used as intermediates in the synthesis of many dyestuffs, such as the Alizarin Saphirols (e.g. Color Constitution No. 63000, 63005, 63010, 63011, 63315 and 63610) can be replaced on an equimolar basis by alpha-di(lower alkoxy)anthraquinones. The alpha-di(lower alkoxy) anthraquinones can be converted in a single step, by treatment with oleum, to the corresponding alpha-dihydroxyanthraquinone-beta-disulfonic acids in almost quantitative yield. The corresponding diamine is obtained by dinitrating followed by reduction of the nitro groups. The known intermediate, leuco 1,4,5,8-tetrahydroxyanthraquinone (see C.I. No. 62500) can be obtained either by reduction of the diamine or by reduction of the dinitro compound. In one embodiment, the alpha-di(lower alkoxy)anthraquinone is obtained from dinitroanthraquinone by treatment thereof with methanol and KOH.