CAS: 3694-52-8; 3-Nitrobenzene-1,2-Diamine

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2,1,3-苯并硒二唑置于盐酸,硫酸,氢碘酸,硝酸体系中,用 水 作为反应溶剂,化学反应 3.5H,反应生成 3-硝基邻苯二胺
参考文献:碱基取代的5'-O-(n-异亮氨酰)氨磺酰基核苷类似物作为潜在的抗菌剂
标题:碱基取代的5'-O-(n-异亮氨酰)氨磺酰基核苷类似物作为潜在的抗菌剂
摘要:氨基酰基氨磺酰基腺苷是体外相应的原核和真核trna合成酶的众所周知的纳摩尔抑制剂.受cubist Pharmaceuticals含芳基四唑的化合物和天然抗生素albomycin中发现的修饰碱基的启发,氨磺酰化腺苷的选择性问题促使我们研究腺嘌呤碱基在药理上的重要性.因此,我们合成并评估了几种异亮氨酰氨磺酰基核苷类似物,它们具有尿嘧啶,胞嘧啶,次黄嘌呤,鸟嘌呤,1,3-二氮杂腺嘌呤(苯并咪唑)或4-硝基苯并咪唑作为杂环碱基.基于微霉素c的结构和抗菌活性,我们还制备了它们的六肽基缀合物,以提高它们的吸收潜力.我们进一步在体外和细胞分析中将它们的抗菌活性与母体异亮氨酰氨磺酰基腺苷(ile-Sa)进行了比较.令人惊讶地,发现含有尿嘧啶类似物的最强的体外抑制作用16楼.不幸的是,由于低吸收,仅发现非常弱的生长抑制特性.根据先前的文献发现对结果进行讨论.
DOI:10.1016/j.Bmc.2014.03.040

专利信息

专利号:US-6251689-B1
优先权日:1998-05-14
标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof
发明人：LABORDE EDGARDO; MATSUMOTO YUKIHARU
权利人:TELIK INC
摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-11053243-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9090661-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2013102730-A1
优先权日:2010-04-02
标 题:Polyamine-containing polymers and methods of synthesis and use
发明人：JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN
权利人:JOST ROBERT W; ULUDAG HASAN; BOLUK MEHMET YAMAN; ALBERTA INNOVATES TECHNOLOGY FUTURES
摘要:The present invention relates to polyamine-containing polymers and methods of their synthesis and use. The polymer may be hydroxyethylcellulose, dextran, poly(vinyl alcohol) or poly(methyl acrylate).

专利号:WO-2020155925-A1
优先权日:2019-01-28
标题:Nitroalkyl quinoxaline or derivative thereof, aminoalkyl quinoxaline or derivative thereof, and synthesis method therefor
发明人：LU QINGHUA; ZHANG SHUYU; LIU TUANQING
权利人:UNIV SHANGHAI JIAOTONG
摘要:The present invention relates to a method for synthesizing a nitroalkyl quinoxaline or a derivative thereof, comprising the following steps: reacting mononitro-substituted o-phenylenediamine or a derivative thereof with nitroalkenyl-substituted benzene or a derivative thereof in a solvent for a predetermined period of time, so as to obtain the nitroalkyl quinoxaline or the derivative thereof. The present application further relates to a nitroalkyl quinoxaline or a derivative thereof. The present application also relates to an aminoalkyl quinoxaline or a derivative thereof, and a preparation method therefor. The method of the present application uses cheap and easily available raw materials, has a simple synthesis process, and the obtained target aminoalkyl quinoxaline or derivative thereof is easy to separate.