2-chloro-5-methylsulfonylthiophene | 98027-41-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 2-chloro-5-methylsulfonylthiophene
• 英文别名: 2-chloro-5-methanesulfonyl-thiophene；2-Chlor-5-methansulfonyl-thiophen；2-Chloro-5-methanesulfonylthiophene
• CAS: 98027-41-9
• 化学式: C₅H₅ClO₂S₂
• mdl: MFCD22741262
• 分子量: 196.678
• InChiKey: QDAMGAJPTWMCGN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  70.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-chloro-5-methylsulfonylthiophene 在 硫酸 、 硝酸 作用下， 生成 2-氯-5-甲基磺酰基-3-硝基噻吩
  参考文献：
  名称：

  2-aminothiophene azo compounds

  摘要：

  公开号：

  US02827450A1
• 作为产物：
  描述：

  5-氯噻唑-2-磺酰氯 、 sodium monochloroacetic acid 在 sodium hydroxide 、 氯乙酸 、 sodium sulfite 作用下， 生成 2-chloro-5-methylsulfonylthiophene
  参考文献：
  名称：

  2-aminothiophene azo compounds

  摘要：

  公开号：

  US02827450A1

文献信息

• [EN] METHYLAMINE DERIVATIVES AS LYSYSL OXIDASE INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE LA MÉTHYLAMINE COMME INHIBITEURS DE LA LYSYL OXIDASE POUR LE TRAITEMENT DU CANCER
  申请人：THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

  公开号：WO2017141049A1

  公开（公告）日：2017-08-24

  Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, wherein W, X, Y, Z, x, R1, R2, R3, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

  提供的是Formula (I)的化合物，或其药用可接受的盐，其中W、X、Y、Z、x、R1、R2、R3、x和n在规范中有定义。这些化合物是赖氨酸氧化酶（LOX）和赖氨酸氧化酶样（LOXL）家族成员（LOXL1、LOXL2、LOXL3、LOXL4）的抑制剂，并且在治疗中很有用，特别是在癌症治疗中。还披露了用于治疗与EGFR相关的癌症的LOX抑制剂，以及预测对LOX抑制剂响应性的生物标志物。
• A novel method for the oxidation of thiophenes. Synthesis of thiophene 1,1-dioxides containing electron-withdrawing substituents
  作者：V. G. Nenajdenko、A. M. Moiseev、E. S. Balenkova

  DOI：10.1007/s11172-005-0107-9

  日期：2004.10

  A novel method for the synthesis of thiophene 1,1-dioxides by oxidation of substituted thiophenes with trifluoroperoxyacetic acid was developed. The effect of the solvent nature on the course of the reaction was studied and optimum conditions for the oxidation of thiophenes containing various functional groups were found. Previously unknown thiophene dioxides were obtained.

  开发了一种通过用三氟过氧乙酸氧化取代噻吩来合成噻吩 1,1-二氧化物的新方法。研究了溶剂性质对反应过程的影响，并找到了氧化含有各种官能团的噻吩的最佳条件。获得了以前未知的噻吩二氧化物。
• A facile route to thiophene-1,1-dioxides bearing electron-withdrawing groups
  作者：Valentine G Nenajdenko、Andrew E Gavryushin、Elizabeth S Balenkova

  DOI：10.1016/s0040-4039(01)00732-8

  日期：2001.6

  thiophene-1,1-dioxides with strong EWGs has been described to date. Trifluoroperacetic acid in acetonitrile in the absence of water is shown to oxidise thiophenes, including examples possessing an electron-withdrawing group such as sulfonyl or alkoxycarbonyl. An easy and ready for scale-up procedure is developed, some formerly unknown thiophene-1,1-dioxides are obtained.

  迄今为止，尚未描述具有强EWG的噻吩-1,1-二氧化物的通用合成方法。乙腈中不存在水的三氟过氧乙酸可氧化噻吩，包括具有吸电子基团的实例，如磺酰基或烷氧基羰基。开发了一种容易且可按比例放大的程序，获得了一些以前未知的噻吩-1,1-二氧化物。
• Methods for preparing sulfonamide substituted alcohols and intermediates thereof
  申请人：Chan Anita Wai-Yin

  公开号：US20070197830A1

  公开（公告）日：2007-08-23

  Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.

  提供了制备氨基醇或其盐以及磺酰胺取代的醇化合物的工艺。理想情况下，磺酰胺取代的醇化合物是杂环磺酰胺三氟烷基取代的醇化合物或苯基磺酰胺三氟烷基取代的醇化合物。
• Substituted pyrazoles as p38 kinase inhibitors
  申请人：Naraian S. Ashok

  公开号：US20070078146A1

  公开（公告）日：2007-04-05

  A class of pyrazole derivatives is described for use in treating p38 kinase medicated disorders. Compounds of particular interest are defined by Formula IA wherein R 1 , R 2 , R 3 and R 4 are as described in the specification.

  描述了一类吡唑衍生物，用于治疗p38激酶介导的疾病。特别感兴趣的化合物由公式IA定义，其中R1、R2、R3和R4如规范中所述。