N-[2-(4-methylphenoxy)ethyl]methanesulfonamide | 928948-39-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: N-[2-(4-methylphenoxy)ethyl]methanesulfonamide
• CAS: 928948-39-4
• 化学式: C₁₀H₁₅NO₃S
• 分子量: 229.3
• InChiKey: QXKSKPUWONPORQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  63.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  甲基磺酰氟 、 2-(4-甲基苯氧基)乙胺 在 三乙胺 作用下， 以 乙腈 为溶剂， 反应 4.0h， 以72%的产率得到N-[2-(4-methylphenoxy)ethyl]methanesulfonamide
  参考文献：
  名称：

  在脂肪族磺酰胺平行合成中，磺酰氟替代磺酰氯

  摘要：

  在平行合成衍生自脂族胺的磺酰胺中，比较了两种类型的脂族磺酰卤（Cl与F）。脂肪族磺酰氟与带有额外官能团的胺显示出良好的效果，而相应的氯化物却不合格。两种磺酰基卤化物在与具有易于接近的氨基的胺的反应中都是有效的。脂肪族磺酰氯与带有空间位阻氨基的胺有效反应，而相应的氟化物显示低活性。

  DOI：

  10.1021/co400164z

文献信息

• NOVEL PYRIDINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2-RECEPTORS
  申请人：Imogai Julien Hassan

  公开号：US20070213323A1

  公开（公告）日：2007-09-13

  The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) X R1 N Y (I) R2 R3 wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是按照公式（I）X R1 N Y（I）R2 R3定义的新型吡啶酮衍生物。该发明的化合物是代谢型受体亚型2（“mGluR2”）的正向变构调节剂，适用于治疗或预防与谷氨酸功能障碍相关的神经系统和精神障碍以及涉及代谢型受体亚型2的疾病。特别是，这些疾病是选择自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的一组。本发明还涉及制备这种化合物和组合物的制药组合物和制备过程，以及利用这种化合物预防和治疗涉及mGluR2的这些疾病的用途。
• METHODS FOR TREATING HEPATITIS C
  申请人：Karp Gary Mitchell

  公开号：US20120009142A1

  公开（公告）日：2012-01-12

  In accordance with the present invention, compounds that inhibit viral replication, preferably Hepatitis C Virus (HCV) replication, have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the treatment or prevention of a viral infection are provided. In another aspect of the invention, compounds useful in the treatment or prevention of HCV infection are provided.

  根据本发明，已经鉴定出抑制病毒复制的化合物，优选地是抑制丙型肝炎病毒（HCV）复制的化合物，并提供了使用这些化合物的方法。在本发明的一个方面，提供了用于治疗或预防病毒感染的化合物。在本发明的另一个方面，提供了用于治疗或预防HCV感染的化合物。
• US7973069B2
  申请人：——

  公开号：US7973069B2

  公开（公告）日：2011-07-05
• US8399493B2
  申请人：——

  公开号：US8399493B2

  公开（公告）日：2013-03-19
• Sulfonyl Fluorides as Alternative to Sulfonyl Chlorides in Parallel Synthesis of Aliphatic Sulfonamides
  作者：Andrey V. Bogolubsky、Yurii S. Moroz、Pavel K. Mykhailiuk、Sergey E. Pipko、Anzhelika I. Konovets、Irina V. Sadkova、Andrey Tolmachev

  DOI：10.1021/co400164z

  日期：2014.4.14

  types of aliphatic sulfonyl halides (Cl versus F) were compared in parallel synthesis of sulfonamides derived from aliphatic amines. Aliphatic sulfonyl fluorides showed good results with amines bearing an additional functionality, while the corresponding chlorides failed. Both sulfonyl halides were effective in the reactions with amines having an easily accessible amino group. Aliphatic sulfonyl chlorides

  在平行合成衍生自脂族胺的磺酰胺中，比较了两种类型的脂族磺酰卤（Cl与F）。脂肪族磺酰氟与带有额外官能团的胺显示出良好的效果，而相应的氯化物却不合格。两种磺酰基卤化物在与具有易于接近的氨基的胺的反应中都是有效的。脂肪族磺酰氯与带有空间位阻氨基的胺有效反应，而相应的氟化物显示低活性。