tosyl sulphonamide | 1035798-56-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: tosyl sulphonamide
• 英文别名: tosyl sulfonamide；TsNH2；Tosylsulfonamide；1-methyl-4-sulfamoylsulfonylbenzene
• CAS: 1035798-56-1
• 化学式: C₇H₉NO₄S₂
• 分子量: 235.285
• InChiKey: OAQLAXKUSRVPDJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  111
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  tosyl sulphonamide 、 1-(pent-4-en-1-yl)-1H-indole-3-carboxylic acid 在 4-二甲氨基吡啶 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 反应 18.0h， 以55%的产率得到1-(pent-4-en-1-yl)-N-tosyl-1H-indole-3-carboxamide
  参考文献：
  名称：

  Pd（II）催化的[4 + 2]杂环序列用于多杂环生成

  摘要：

  报道了一种新的Pd（II）催化的级联序列，用于从简单的起始原料形成多杂环。该序列适用于吲哚和吡咯底物，并且可以接受一定范围的取代基。该反应被认为是通过Pd（II）催化的C–H活化的Heck反应进行的，然后是第二个Pd（II）催化的aza-Wacker反应，每个序列有两个Cu（II）介导的Pd（0）转换。该序列可以被认为是正式的[4 + 2]杂环化。

  DOI：

  10.1021/acs.orglett.8b02543

文献信息

• [EN] CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME<br/>[FR] COMPOSÉS CYTOTOXIQUES ET ANTIMITOTIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：CT FOR DRUG RES AND DEV

  公开号：WO2014144871A1

  公开（公告）日：2014-09-18

  Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

  揭示了具有细胞毒性和/或抗有丝分裂活性的化合物。还揭示了与制备和使用这些化合物相关的方法，以及包含这些化合物的药物组合物。还揭示了具有结构的组合物：(T)-(L)-(D)，其中(T)是靶向基团，(L)是可选的连接物，(D)是具有细胞毒性和/或抗有丝分裂活性的化合物。
• Efficient aziridination of olefins catalyzed by dirhodium catalysts
  申请人：Doyle P. Michael

  公开号：US20060211870A1

  公开（公告）日：2006-09-21

  This invention relates to compositions and methods for achieving the efficient aziridination of organic molecules, especially olefins. More specifically, the invention is directed to a mild, selective, and efficient aziridination protocol that involves catalysis by a mixed-valent dirhodium(II,III) catalyst (Rh 2 5+ ). Especially preferred sources for forming such mixed-valent dirhodium(II,III) catalyst (Rh 2 5+ ) are dirhodium(II) carboxamidates, such as dirhodium(II) caprolactamate, and their derivatives and analogues.

  这项发明涉及用于实现有机分子，特别是烯烃的高效环氮化的组合物和方法。更具体地，该发明涉及一种温和、选择性和高效的环氮化方案，涉及通过混合价二铑（II,III）催化剂（Rh25+）进行催化。特别偏好用于形成这种混合价二铑（II,III）催化剂（Rh25+）的来源是二铑（II）羧酰胺酸盐，例如二铑（II）己内酰胺酸盐，以及它们的衍生物和类似物。
• [EN] STAT3 DIMERIZATION INHIBITORS<br/>[FR] INHIBITEURS DE DIMÉRISATION DE STAT3
  申请人：H LEE MOFFITT CANCER CT & RES

  公开号：WO2014070859A1

  公开（公告）日：2014-05-08

  The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

  本文所披露的主题涉及组成物的制备和使用方法。在进一步的方面，本文所披露的主题涉及STAT3二聚化抑制剂。还揭示了制备这些组成物的方法以及包含这些组成物的组合物。还揭示了通过向需要的个体投与所披露的化合物的有效量来治疗或预防某些癌症的方法。此外，本文还揭示了通过将细胞与本文所披露的化合物或组合物接触以抑制STAT3的方法。
• METHOD FOR PRODUCING PEPTIDE THIOESTER
  申请人：Manabe Shino

  公开号：US20090240034A1

  公开（公告）日：2009-09-24

  It is an object of the present invention to provide a novel method for producing a peptide thioester. In the present invention, general peptide synthesis is performed on a solid-phase resin, carboxylic acid obtained after cutout is allowed to react with p-toluenesulfonyl isocyanate, and then the reaction product is alkylated, and is reacted with thiol. Thus, peptide thioester is simply synthesized under mild conditions.

  本发明的目的是提供一种新型的肽硫酸酯生产方法。在本发明中，一般的肽合成是在固相树脂上进行的，剪切后得到的羧酸与对甲苯磺酰异氰酸酯反应，然后将反应产物烷基化，并与巯基反应。因此，在温和的条件下简单地合成了肽硫酸酯。
• Antioxidant Small Molecules Aimed at Targeting Metal-Based Oxidative Stress in Neurogenerative Disorders
  申请人：Texas Christian University

  公开号：US20140206862A1

  公开（公告）日：2014-07-24

  Amine chelates capable of antioxidant capacity and amyloid disaggregation are shown which may be useful in targeting metal-based oxidative stress in neurodegenerative disorders. Pyclen, a backbone commonly investigated for contrast agent imaging, may be repurposed as an anti-oxidant chelator for disaggregating amyloid. The antioxidant capacity of pyclen is enhanced dramatically via conversion of the pyridine backbone to a pyridol with cellular studies showing superior antioxidant capacity while retaining chelation ability to protect amyloid from metal ions aggregation and also disaggregate amyloid aggregates. Another family of molecules based upon hybrid heterocyclic amine ligands is also presented.

  展示了具有抗氧化能力和淀粉样蛋白解聚能力的胺螯合物，这可能有助于针对神经退行性疾病中基于金属的氧化应激进行靶向治疗。Pyclen是一种常用于对比剂成像的骨架，可以重新用作抗氧化剂螯合剂，用于解聚淀粉样蛋白。通过将吡啶骨架转化为吡啶醇，可以显著增强pyclen的抗氧化能力，并通过细胞研究表明其具有更优越的抗氧化能力，同时保留了保护淀粉样蛋白免受金属离子聚集和解聚淀粉样蛋白聚集的螯合能力。还介绍了另一族基于杂环胺配体的分子。