N-(5-acetyl-2-fluoro-phenyl)-N-methyl-methanesulfonamide | 920751-47-9

• 英文名称: N-(5-acetyl-2-fluoro-phenyl)-N-methyl-methanesulfonamide
• 英文别名: N-(5-acetyl-2-fluorophenyl)-N-methylmethanesulfonamide
• CAS: 920751-47-9
• 化学式: C₁₀H₁₂FNO₃S
• 分子量: 245.275
• InChiKey: JCNWUMZBAMNZMQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  62.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-(5-acetyl-2-fluoro-phenyl)-N-methyl-methanesulfonamide 、 N,N-二甲基甲酰胺二甲基缩醛 反应 2.5h， 以67.4%的产率得到N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-methanesulfonamide
  参考文献：
  名称：

  Halogenated pyrazolo[1,5-a]pyrimidines, processes, uses, compositions and intermediates

  摘要：

  该发明提供了式（I）的新型卤代吡唑并[1,5-a]嘧啶化合物，其中R、R1、X和Y具有不同的含义，以及其药学上可接受的盐。式（I）的化合物可用于治疗或预防焦虑症、癫痫和睡眠障碍，包括失眠，并诱导镇静-催眠、麻醉、睡眠和肌肉松弛。该发明还提供了用于制备所述化合物和某些中间体的合成方法，以及中间体本身。

  公开号：

  EP1736475A1

文献信息

• Halogenated Pyrazolo[1,5-A]Pyrimidines, Processes, Uses, Compositions and Intermediates
  申请人：Anglada Luis

  公开号：US20090111848A1

  公开（公告）日：2009-04-30

  The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R 1 , X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

  本发明提供了式（I）的新型卤代吡唑并[1,5-a]嘧啶，其中R，R1，X和Y具有不同的含义，以及其药学上可接受的盐。式（I）的化合物用于治疗或预防焦虑症、癫痫和睡眠障碍，包括失眠，并用于诱导镇静-催眠、麻醉、睡眠和肌肉松弛。本发明还提供了制备所述化合物和某些中间体的合成方法，以及中间体本身。
• Halogenated pyrazolo[1,5-A]pyrimidines, processes, uses, compositions and intermediates
  申请人：Anglada Luis

  公开号：US08530482B2

  公开（公告）日：2013-09-10

  The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

  该发明提供了式（I）的新型卤代吡唑并[1,5-a]嘧啶化合物，其中R，R1，X和Y具有不同的含义，以及其药学上可接受的盐。式（I）的化合物可用于治疗或预防焦虑症，癫痫和睡眠障碍，包括失眠，并用于诱导镇静-催眠，麻醉，睡眠和肌肉松弛。该发明还提供了用于制备所述化合物和某些中间体的合成方法，以及中间体本身。
• Method of treating insomnia with halogenated pyrazolo[1,5-a]pyrimidines
  申请人：FERRER INTERNACIONAL, S.A.

  公开号：US10072000B2

  公开（公告）日：2018-09-11

  The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R1, X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.

  本发明提供了式(I)的新型卤代吡唑并[1,5-a]嘧啶，其中R、R1、X和Y具有不同的含义，以及其药学上可接受的盐类。式（I）化合物可用于治疗或预防焦虑、癫痫和包括失眠在内的睡眠障碍，以及诱导镇静催眠、麻醉、睡眠和肌肉放松。本发明还提供了制备上述化合物和某些中间体以及中间体本身的合成程序。
• HALOGENATED PYRAZOLO [1,5-A]PYRIMIDINES, PROCESSES, USES AS GABA-A RECEPTORS LIGAND, COMPOSITIONS AND INTERMEDIATES
  申请人：Ferrer Internacional, S.A.

  公开号：EP1899343A1

  公开（公告）日：2008-03-19
• HALOGENATED PYRAZOLO[1,5-A]PYRIMIDINES, PROCESSES, USES, COMPOSITIONS AND INTERMEDIATES
  申请人：Ferrer Internactional, S.A.

  公开号：US20160368912A9

  公开（公告）日：2016-12-22

  The invention provides novel halogenated pyrazolo[1,5-a]pyrimidines of formula (I) wherein R, R 1 , X and Y have different meanings, and pharmaceutically acceptable salts thereof. Compounds of formula (I) are useful for treating or preventing anxiety, epilepsy and sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.