CAS: 97997-76-7; 2,4,5,6-Tetramethylbenzene-1,3-Disulfonyl Dichloride

该化合物是一种化学化合物,其结构特征包括两组附属于四甲基代苯环的氯基磺酸盐,在室温下,这种化合物一般没有色状,可粉黄,在室内温度下是固体的,由于存在氯基磺化物功能组,其极强的电益特性而闻名;这种化合物反应性很强,特别是核糖核,使其在有机合成中有用,特别是在形成磺酰胺衍生物和其他含磺酰氟化合物时;该化合物也是湿质的,这意味着它可以吸收空气中的水分,这可能影响其稳定性和再活性;在处理这种物质时,必须采取安全防范措施,因为它可以是腐蚀性的,并可能导致皮肤,眼睛和呼吸系统受到刺激;在冷,干燥,远离水分和不相容物质的地方适当储存,对于保持其化学反应的完整性和有效性至关重要.

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1,2,3,5-Tetramethylbenzene 4-{[3-(4-tert-butylphenylsulfamoyl)-2,4,5,6-tetramethylbenzenesulfonylamino]methyl}piperidine-1-carboxylic acid tert-butyl ester

合成工艺路线路线简述

  • 合成目标产物 2,4,5,6-Tetramethylbenzenedisulfonyl Dichloride 主要起始原料 1,2,3,5-Tetramethylbenzene
  • (文献来源)合成步骤主要原料 1,2,3,5-Tetramethylbenzene
📜1,2,3,5-四甲基苯置于氯磺酸体系中,用48%的收率获得产物2,4,5,6-四甲基苯二磺酸氯
参考文献:通过磷酸三酯方法使用s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯和双功能缩合试剂合成寡脱氧核糖核苷酸
标题:通过磷酸三酯方法使用s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯和双功能缩合试剂合成寡脱氧核糖核苷酸
摘要:合成了四种芳香二磺酰氯作为寡聚脱氧核糖核苷酸合成的缩合剂,并在胸苷基(3'-5')胸腺嘧啶核苷的合成中考察了它们的缩合能力.其中,均三甲苯二磺酰氯(mds)和异二烯丙基异磺酰氯(dds)被证明对于缩合和从同时形成的5'-磺化副产物中分离产物是有效的.本文详细描述了通过次膦酸酯从s,S-二苯基脱氧核糖核苷3'-磷酸二硫酯衍生物中选择性除去两个苯硫基之一的研究,这些衍生物已成功地用作液相合成十二烷氧基核糖核苷酸的起始结构单元,Dcattattaatac.
DOI:10.1016/s0040-4020(01)96778-X

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专利信息


专利号:US-2009111737-A1
优先权日:1999-05-24
标题:Novel antibacterial agents
发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

专利号:US-7179794-B2
优先权日:1998-06-08
标题 :Multivalent macrolide antibiotics
发明人:GRIFFIN JOHN H; PACE JOHN L
权利人:THERAVANCE INC
摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.

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合成参考文献

参考DOI号:10.1016/S0040-4020(01)96778-X
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