3-Amino-N-[4-(trifluoromethyl)phenyl]benzamide | 1011244-73-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-Amino-N-[4-(trifluoromethyl)phenyl]benzamide
• CAS: 1011244-73-7
• 化学式: C₁₄H₁₁F₃N₂O
• 分子量: 280.249
• InChiKey: VVJKTSKZDFTNKL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-Amino-N-[4-(trifluoromethyl)phenyl]benzamide 、 二甲胺基磺酰氯 在 吡啶 作用下， 反应 1.5h， 生成 3-(dimethylsulfamoylamino)-N-[4-(trifluoromethyl)phenyl]benzamide
  参考文献：
  名称：

  Synthesis and antiviral activity of sulfonamidobenzophenone oximes and sulfonamidobenzamides

  摘要：

  To find antiviral agents, various sulfonamidobenzophenone oximes (II) were synthesized from the appropriate m-sulfonamidobenzophenones by hydroxylamine reaction. The reaction products were generally obtained as syn/anti mixtures which were separable by fractional crystallization. The anti isomer had more potent antipoliovirus activity than the syn isomer. Various sulfonamidobenzamides (III) which were structurally related to II were synthesized by the reactions of amino-substituted benzamides with sulfuryl chloride or amines with (aminosulfonyl)benzoyl chloride. Antiviral activity was examined by the plaque-inhibition test. Compounds 5, 36, and 69 exhibited strong antipicornavirus activity. The structure-activity relationships are discussed.

  DOI：

  10.1021/jm00153a018
• 作为产物：
  描述：

  间硝基苯甲酰氯 在 盐酸 、 tin 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 1.08h， 生成 3-Amino-N-[4-(trifluoromethyl)phenyl]benzamide
  参考文献：
  名称：

  Synthesis and antiviral activity of sulfonamidobenzophenone oximes and sulfonamidobenzamides

  摘要：

  To find antiviral agents, various sulfonamidobenzophenone oximes (II) were synthesized from the appropriate m-sulfonamidobenzophenones by hydroxylamine reaction. The reaction products were generally obtained as syn/anti mixtures which were separable by fractional crystallization. The anti isomer had more potent antipoliovirus activity than the syn isomer. Various sulfonamidobenzamides (III) which were structurally related to II were synthesized by the reactions of amino-substituted benzamides with sulfuryl chloride or amines with (aminosulfonyl)benzoyl chloride. Antiviral activity was examined by the plaque-inhibition test. Compounds 5, 36, and 69 exhibited strong antipicornavirus activity. The structure-activity relationships are discussed.

  DOI：

  10.1021/jm00153a018

文献信息

• [EN] NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS<br/>[FR] NOUVEAUX INHIBITEURS À PETITES MOLÉCULES DE FACTEURS DE TRANSCRIPTION TEAD
  申请人：MASSACHUSETTS GEN HOSPITAL

  公开号：WO2020190774A1

  公开（公告）日：2020-09-24

  The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.

  本公开涉及化合物及其组合物和使用方法。这些化合物抑制TEAD转录因子的活性，并可用于治疗与TEAD转录因子活性相关的疾病，例如癌症和其他疾病。
• Liquid crystal orienting agent
  申请人：JAPAN SYNTHETIC RUBBER CO., LTD.

  公开号：EP0735403A1

  公开（公告）日：1996-10-02

  A liquid crystal aligning agent contains (1) at least one polymer selected from the group consisting of a polyamic acid obtainable by a reaction between a tetracarboxylic acid dianhydride and a diamine compound and an imidized polymer obtainable by cyclization with dehydration of the polyamic acid; (2) at least one first solvent selected from the group consisting of N-alkyl-2-pyrrolidones, lactones, and 1,3-dialkyl-2-imidazolidinones; (3) at least one second solvent selected from the group consisting of: (a) a first compound represented by general formula (I) wherein R1 is an alkylene group having 2 or 3 carbon atoms; R2 is an alkyl group having 1 to 4 carbon atoms an acetyl group or a propionyl group; R3 is an alkyl group having 1 to 3 carbon atoms, an alkoxyl group having 1 to 3 carbon atoms, or a halogen atom; a is 1 or 2; and b is 0 or integers of from 1 to 5; and (b) a second compound represented by general formula (II) wherein R4 is an alkyl group having 1 to 4 carbon atoms; R5 is an alkylene group having 2 or 3 carbon atoms; R6 is an alkyl group having 1 to 3 carbon atoms; and c is 1 or 2.

  液晶对准剂包含 (1) 至少一种聚合物，选自由四羧酸二酐和二胺化合物反应生成的聚氨基 酸和聚氨基酸脱水环化生成的亚胺化聚合物组成的组； (2) 至少一种第一溶剂，选自由 N-烷基-2-吡咯烷酮、内酯和 1,3-二烷基-2-咪唑烷酮组成的组； (3) 至少一种第二溶剂，选自由下列物质组成的组 (a) 通式 (I) 所代表的第一种化合物 其中 R1 是具有 2 或 3 个碳原子的亚烷基；R2 是具有 1 至 4 个碳原子的烷基、乙酰基或丙酰基；R3 是具有 1 至 3 个碳原子的烷基、具有 1 至 3 个碳原子的烷氧基或卤原子；a 是 1 或 2；b 是 0 或 1 至 5 的整数；以及 (b) 通式(II)代表的第二种化合物 其中 R4 是具有 1 至 4 个碳原子的烷基；R5 是具有 2 或 3 个碳原子的亚烷基；R6 是具有 1 至 3 个碳原子的烷基；以及 c 是 1 或 2。
• Cyclooxygenase-1-Selective Inhibitors Are Attractive Candidates for Analgesics That Do Not Cause Gastric Damage. Design and in Vitro/in Vivo Evaluation of a Benzamide-Type Cyclooxygenase-1 Selective Inhibitor
  作者：Hiroki Kakuta、Xiaoxia Zheng、Hiroyuki Oda、Shun Harada、Yukio Sugimoto、Kenji Sasaki、Akihiro Tai

  DOI：10.1021/jm701191z

  日期：2008.4.1

  Although cyclooxygenase-1 (COX-1) inhibition is thought to be a major mechanism of gastric damage by nonsteroidal anti-inflammatory drugs (NSAIDs), some COX-1-selective inhibitors exhibit strong analgesic effects without causing gastric damage. However, it is not clear whether their analgesic effects are attributable to COX-1-inhibitory activity or other bioactivities. Here, we report that N-(5-amino-2-pyridinyl)-4(trifluoromethyl)benzamide (18f, TFAP), which has a structure clearly different from those of currently available COX-1-selective inhibitors, is a potent COX-1-selective inhibitor (COX-1IC(50) = 0.80 +/- 0.05 mu M, COX-2IC(50) = 210 I mu M). This compound causes little gastric damage in rats even at an oral dose of 300 mg/kg, though it has an analgesic effect at as low a dose as 10 mg/kg. Our results show that COX-1-selective inhibitors can be analgesic agents without causing gastric damage.
• OGATA, MASARU;MATSUMOTO, HIROSHI;SHIMIZU, SUMIO;KIDA, SHIRO;WADA, TORU;SH+, J. MED. CHEM., 1986, 29, N 3, 417-423
  作者：OGATA, MASARU、MATSUMOTO, HIROSHI、SHIMIZU, SUMIO、KIDA, SHIRO、WADA, TORU、SH+

  DOI：——

  日期：——
• US5700860A
  申请人：——

  公开号：US5700860A

  公开（公告）日：1997-12-23