3-methyl-6-trifluoromethyl-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide | 723-57-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻二嗪
• 英文名称: 3-methyl-6-trifluoromethyl-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
• 英文别名: 4H-1,2,4-Benzothiadiazine, 3-methyl-6-trifluoromethyl-, 1,1-dioxide；3-methyl-6-(trifluoromethyl)-4H-1λ6,2,4-benzothiadiazine 1,1-dioxide
• CAS: 723-57-9
• 化学式: C₉H₇F₃N₂O₂S
• 分子量: 264.228
• InChiKey: YLOIUIYEPKSXIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  66.9
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  盐酸乙脒 、 2-溴-4-(三氟甲基)苯磺酸 在 caesium carbonate 、 copper(I) bromide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 0.17h， 以77%的产率得到3-methyl-6-trifluoromethyl-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
  参考文献：
  名称：

  2-卤代苯磺酰胺与Am的铜催化合成1,2,4-苯并噻二嗪1,1-二氧化物衍生物

  摘要：

  我们已经开发了一种简单实用的铜催化方法，该方法通过取代的2-卤代苯磺酰胺与am的级联反应来合成1,2,4-苯并噻二嗪1,1-二氧化物衍生物，该方法对于构建这种化合物具有重要的价值。一种具有生物学和医学活性的分子。

  DOI：

  10.1002/adsc.200900101

文献信息

• Hair growth stimulation with nitroxide and other radicals
  申请人：PROCTOR, Peter H.

  公开号：EP0327263A1

  公开（公告）日：1989-08-09

  Hair growth stimulation with nitroxide and other radicals. A nitroxide radical source compound is applied topically with an adjuvant selected from reducing agents, hydroxyl radical scavengers and antioxidants to activate formation of the nitroxide radical and/or to protect the nitroxide radical from reaction with other free radicals. Also disclosed is a kit for preparing a unit dose for topical application of a nitric oxide generating compound and a reducing agent reactive therewith to form nitric oxide on or in the skin. Other adjuvants include SOD and antiandrogens. Various other radical-­forming hair growth stimulants and preparations thereof are disclosed.

  用亚硝基和其他自由基刺激头发生长。一氧化氮自由基源化合物与选自还原剂、羟自由基清除剂和抗氧化剂的辅助剂一起局部施用，以激活一氧化氮自由基的形成和/或保护一氧化氮自由基不与其他自由基发生反应。 还公开了一种试剂盒，用于制备单位剂量的一氧化氮生成化合物和与之反应在皮肤上或皮肤内形成一氧化氮的还原剂，供局部使用。其他辅助剂包括 SOD 和抗雄激素。还公开了其他各种自由基生发刺激剂及其制剂。
• USE OF DIAZOXIDE FOR SUPPRESSING THE PLASMA INSULIN LEVEL IN A MAMMAL
  申请人：De Boer Johannes Mathijs Maria

  公开号：US20100234362A1

  公开（公告）日：2010-09-16

  The present invention relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof, wherein the fasting and/or postabsorptive plasma insulin level is reduced to about 5 mU/l or less. The present invention also relates to the use of a potassium channel activator in the manufacture of a medicament for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising orally administering to said mammal in need thereof a daily dosage of about 5 mg to about 1200 mg, calculated on a Diazoxide active weight basis.
• USE OF A COMBINATION OF DIAZOXIDE AND METFORMIN FOR TREATING OBESITY OR OBESITY RELATED DISORDERS
  申请人：De Boer Johannes Marthijs Maria

  公开号：US20120053172A1

  公开（公告）日：2012-03-01

  The present invention relates to a method for suppressing the fasting plasma insulin level and/or postabsorptive insulin level in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug. The present invention also relates to a method for treating or preventing obesity, obesity related disorders and conditions and other disorders and conditions related to weight gain in a mammal in need thereof, said method comprising administering to said mammal a pharmaceutically effective amount of a combination of a potassium channel activator and an anti-diabetic drug.
• [EN] TOPICAL COMPOSITION FOR STIMULATING HAIR GROWTH WITH STABLE FREE RADICALS
  申请人：PROCTOR, Peter, H.

  公开号：WO1988005653A1

  公开（公告）日：1988-08-11

  (EN) Topical composition and method for stimulating hair growth. The composition contains, in an occlusive or semiocclusive pharmaceutical carrier, a stable free radical forming substance such as minoxidil, diphenyl hydantoin, diazoxide, porphyrin, proxyl, doxyl or tempo, an antiandrogen such as spironolactone, and optimally, a free radical scavenger such as dimethyl sulfoxide, a tertiary phosphine oxide or a retinoid. The method involves applying the composition to skin, preferably water-soaked skin, once or twice a day.(FR) Composition à application locale et procédé de stimulation de la croissance des cheveux. La composition contient dans un excipient pharmaceutique occlusif ou semi-occlusif une substance formant des radicaux libres stables, telle que minoxydil, diphényle, hydantoïne, diazoxyde, porphyrine, proxyle, doxyle ou tempo, un anti-androgène tel que sprinolactone, et de préférence, un suppresseur de radicaux libres tels que le diméthyl sulfoxyde, un oxyde de phosphine tertiaire ou un rétinoïde. Le procédé consiste à appliquer la composition sur la peau, de préférence la peau mouillée avec de l'eau, une ou deux fois par jour.
• Copper-Catalyzed Synthesis of 1,2,4-Benzothiadiazine 1,1-Dioxide Derivatives by Coupling of 2-Halobenzenesulfonamides with Amidines
  作者：Daoshan Yang、Hongxia Liu、Haijun Yang、Hua Fu、Liming Hu、Yuyang Jiang、Yufen Zhao

  DOI：10.1002/adsc.200900101

  日期：——

  We have developed a simple and practical copper-catalyzed method for the synthesis of 1,2,4-benzothiadiazine 1,1-dioxide derivatives via cascade reactions of substituted 2-halobenzenesulfonamides with amidines, and the method is of value for the construction of this kind of molecules with biological and medicinal activities.

  我们已经开发了一种简单实用的铜催化方法，该方法通过取代的2-卤代苯磺酰胺与am的级联反应来合成1,2,4-苯并噻二嗪1,1-二氧化物衍生物，该方法对于构建这种化合物具有重要的价值。一种具有生物学和医学活性的分子。