4-bromo-N-(pyridin-2-yl)-2-(trifluoromethyl)benzamide | 1299483-06-9

• 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: 4-bromo-N-(pyridin-2-yl)-2-(trifluoromethyl)benzamide
• 英文别名: 4-bromo-N-pyridin-2-yl-2-(trifluoromethyl)benzamide
• CAS: 1299483-06-9
• 化学式: C₁₃H₈BrF₃N₂O
• 分子量: 345.119
• InChiKey: VOASXWGOMSYNGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  methyl 3-ethynyl-5-fluorobenzoate 、 4-bromo-N-(pyridin-2-yl)-2-(trifluoromethyl)benzamide 在 bis-triphenylphosphine-palladium(II) chloride 、 copper(l) iodide 、 三乙胺 作用下， 以 乙酸乙酯 为溶剂， 反应 2.0h， 以74%的产率得到3-fluoro-5-[3-(pyridin-2-ylcarbamoyl)-4-trifluoromethylphenylethynyl]benzoic acid methyl ester
  参考文献：
  名称：

  [EN] ETHYNYL COMPOUNDS, THEIR PREPARATION AND THEIR THERAPEUTIC USE FOR THE TREATMENT OF MALARIA
  [FR] COMPOSÉS ÉTHYNYLE, LEUR PRÉPARATION ET LEUR UTILISATION THÉRAPEUTIQUE DANS LE TRAITEMENT DU PALUDISME

  摘要：

  本公开涉及式(I)的化合物或其药用盐，其中R1表示氟原子或含有1、2或3个碳原子的全卤线性烷基基团；R2表示氯原子、含有1、2或3个碳原子的线性烷基基团或含有1、2或3个碳原子的全卤线性烷基基团，R表示氢原子或式(la)的基团。本公开还涉及它们的制备方法以及它们的治疗用途，特别是用于治疗疟疾。

  公开号：

  WO2019008027A1

文献信息

• Haloalkyl-substituted amides as insecticides and acaricides
  申请人：HEIL Markus

  公开号：US20110105532A1

  公开（公告）日：2011-05-05

  The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R 1 to R 6 , Q 1 to Q 8 , A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.

  本发明涉及一般式（I）中卤代酰胺衍生物，其中R1至R6、Q1至Q8、A、V、W、X、Y、n和m如描述中所述定义，并涉及其制备方法以及作为杀虫剂和杀螨剂的用途。
• Haloalkyl-Substituted Amides as Insecticides and Acaricides
  申请人：Heil Markus

  公开号：US20130172390A1

  公开（公告）日：2013-07-04

  The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R 1 to R 6 , Q 1 to Q 8 , A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.

  本发明涉及一般式(I)的卤代酰胺衍生物，其中R1到R6、Q1到Q8、A、V、W、X、Y、n和m的定义如描述中所述，以及其制备过程和用作杀虫剂和杀螨剂的用途。
• Ethynyl compounds, their preparation and their therapeutic use for the treatment of malaria
  申请人：SANOFI

  公开号：US11078160B2

  公开（公告）日：2021-08-03

  The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 means a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; R2 means a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (Ia). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria.

  本公开涉及式 (I) 的化合物或其药学上可接受的盐，其中 R1 指氟原子或含有 1、2 或 3 个碳原子的全卤代直链烷基；R2 指氯原子、含有 1、2 或 3 个碳原子的直链烷基或含有 1、2 或 3 个碳原子的全卤代直链烷基，R 指氢原子或式 (Ia) 的基。本公开还涉及其制备工艺及其治疗用途，特别是用于治疗疟疾等。
• HALOGENALKYL-SUBSTITUIERTE AMIDE ALS INSEKTIZIDE UND AKARIZIDE
  申请人：Bayer CropScience AG

  公开号：EP2493844A2

  公开（公告）日：2012-09-05
• ETHYNYL COMPOUNDS, THEIR PREPARATION AND THEIR THERAPEUTIC USE FOR THE TREATMENT OF MALARIA
  申请人：SANOFI

  公开号：US20200281909A1

  公开（公告）日：2020-09-10

  The present disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 means a fluorine atom or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms; R 2 means a chlorine atom, a linear alkyl radical containing 1, 2 or 3 carbon atoms or a perhalogeno linear alkyl radical containing 1, 2 or 3 carbon atoms, and R means a hydrogen atom or a radical of formula (Ia). The present disclosure also relates to processes for their preparation as well their therapeutic uses, in particular such as for use in the treatment of malaria.