4-氯-2,5-二氟苯磺酰氯 | 286932-78-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-氯-2,5-二氟苯磺酰氯
• 英文名称: 4-chloro-2,5-difluorophenylsulfonyl chloride
• 英文别名: 4-Chloro-2,5-difluorobenzenesulfonyl chloride
• CAS: 286932-78-3
• 化学式: C₆H₂Cl₂F₂O₂S
• mdl: MFCD02091386
• 分子量: 247.049
• InChiKey: RONRQDJNXCXAOU-UHFFFAOYSA-N

物化性质

• 沸点：
  253.1±35.0 °C(Predicted)
• 密度：
  1.686±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42.5
• 氢给体数：
  0
• 氢受体数：
  4

安全信息

• 危险等级：
  CORROSIVE
• 海关编码：
  2904909090

反应信息

• 作为反应物：
  描述：

  4-氯-2,5-二氟苯磺酰氯 在 三乙胺 作用下， 以 吡啶 、 乙腈 为溶剂， 反应 0.42h， 生成 Anthranilic Acid Sulfonamide, 10aj
  参考文献：
  名称：

  Discovery and Optimization of Anthranilic Acid Sulfonamides as Inhibitors of Methionine Aminopeptidase-2:  A Structural Basis for the Reduction of Albumin Binding

  摘要：

  Methionine aminopeptidase-2 (MetAP2) is a novel target for cancer therapy. As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening. These micromolar hits were rapidly improved to nanomolar leads on the basis of insights from protein crystallography; however, the compounds displayed extensive binding to human serum albumin and had limited activity in cellular assays. Modifications based on structural information on the binding of lead compounds to both MetAP2 and domain III of albumin allowed the identification of compounds with significant improvements in both parameters, which showed good cellular activity in both proliferation and methionine processing assays.

  DOI：

  10.1021/jm0601001

文献信息

• Inhibitors of cytosolic phospholipase A2
  申请人：Wyeth

  公开号：US20030144282A1

  公开（公告）日：2003-07-31

  This invention provides substituted indole compounds of the general formula: 1 and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A 2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

  这项发明提供了一般式如下的取代吲哚化合物： 1 及其药用可接受的盐形式，以及将这些化合物用作各种磷脂酶酶的抑制剂的方法，特别是磷脂酶A 2 酶，并用于医疗治疗、预防和抑制疼痛和炎症。
• BENZOCYCLOHEPTENE ACETIC ACIDS
  申请人：Firooznia Fariborz

  公开号：US20120309796A1

  公开（公告）日：2012-12-06

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.

  本文提供的是化合物的公式(I)以及其药用盐，其中取代基如规范中所披露的那样。这些化合物及含有它们的药物组合物对于治疗炎症性疾病和紊乱，如哮喘和慢性阻塞性肺病等，具有用处。
• Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
  申请人：Clerin Valerie

  公开号：US20080009485A1

  公开（公告）日：2008-01-10

  This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.

  这项发明提供了一种使用通式所示的取代吲哚化合物及其药用盐形式的方法。该发明提供了一种在哺乳动物中治疗或预防血栓形成，或预防血栓形成症状进展的化合物使用方法。
• Novel indazolone derivatives useful as 11b-HSD1 inhibitors
  申请人：Amrein Kurt

  公开号：US20060069269A1

  公开（公告）日：2006-03-30

  Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 7 have the significances given in the description and claims can be used in the form of pharmaceutical compositions.

  化合物的公式为（I），以及其药用盐和酯，其中R1到R7具有描述和索赔中给出的含义，可以用于制备药物组合物。
• Methods for treating arthritic disorders
  申请人：Wyeth

  公开号：US20030166649A1

  公开（公告）日：2003-09-04

  This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: 1 and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A 2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

  本发明提供了一种使用一般式（1）的取代吲哚化合物及其药学上可接受的盐形式来治疗哺乳动物的关节炎或风湿性疾病的方法，以及使用这些化合物作为各种磷脂酶酶活性抑制剂，特别是磷脂酶A2酶的抑制剂的方法，并用于医疗治疗、预防和抑制疼痛和炎症。