(E)-1-(cyclohexylmethylene)-2-phenylhydrazine

• 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: (E)-1-(cyclohexylmethylene)-2-phenylhydrazine
• 英文别名: N-[(E)-cyclohexylmethylideneamino]aniline
• 化学式: C₁₃H₁₈N₂
• 分子量: 202.299
• InChiKey: ULQNPPZPCPKGAQ-SDNWHVSQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  24.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (E)-1-(cyclohexylmethylene)-2-phenylhydrazine 、 苯胺 在 盐酸 、 sodium nitrite 、 吡啶 作用下， 以 水 为溶剂， 反应 2.5h， 生成
  参考文献：
  名称：

  Anti-Plasmodium activity of tetrazolium salts

  摘要：

  We have previously reported that sulfated cyclodextrins inhibit the invasion of Plasmodium merozoites by interacting with receptors present on the surface of erythrocytes. The observation that tetrazolium salts formed stable complexes with the inhibitory sulfated cyclodextrins suggested that tetrazolium salts might have anti-Plasmodium activity as well. Evaluation of commercially available tetrazolium salts indicated that some were active in the low nanomolar range and showed specificity in their inhibition of Plasmodium. Synthesis of a further 54 structures allowed us to determine that activity results from an aromatic component attached to the tetrazolium carbon atom (R-1) and its size is not critical to the activity of the compound. Nitro modi. cations of active compounds are poorly tolerated, however, the presence of halogen atoms on aromatic groups attached to the nitrogen atoms of the tetrazolium ring (R-2 and R-3) has little effect on activity. Methoxy groups are tolerated on R-2 and R-3 components; however, they are disruptive on the R-1 component. The overall results suggest that the R-1 component is interacting with a specific hydrophobic environment and the R-2 and R-3 components are less constrained. The activity of these compounds in several human and mouse Plasmodium cultures suggests that the compounds interact with a component of the parasite that is both essential and conserved. (c) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.11.005
• 作为产物：
  描述：

  苯肼 、 环己烷基甲醛 在 N-甲基-D-葡胺 作用下， 以 乙醇 、 水 为溶剂， 反应 0.67h， 以86%的产率得到(E)-1-(cyclohexylmethylene)-2-phenylhydrazine
  参考文献：
  名称：

  葡甲胺催化羰基化合物和酰肼合成腙的简单有效方法

  摘要：

  摘要 在葡甲胺存在的情况下，在室温下，在乙醇水溶液中，已经开发出一种简单、环境友好的方案，用于从羰基化合物和酰肼合成腙。本协议的显着特点是反应条件温和、反应时间短、产量高、操作简单、不含金属、适用于大规模合成以及可生物降解且价格低廉的催化剂。图形概要

  DOI：

  10.1080/00397911.2016.1258476

文献信息

• Indole derivatives, process for their preparation and pharmaceutical compositions containing them
  申请人：BEECHAM GROUP PLC

  公开号：EP0287196A1

  公开（公告）日：1988-10-19

  Compounds of formula (I), or a pharmaceutically acceptable salt thereof: wherein     L is NH or O;     R₁ is hydrogen, fluoro or chloro;     R₂ and R₅ are independently hydrogen or C₁₋₆ alkyl or together are a bond; or     R₂ and R₃ and/or R₄ and R₅, together are C₂₋₇ polymethylene or-(CH₂)m-O-(CH₂)x- where m and x are 1 to 5 such that m+x is 2 to 6;     R₄ is C₁₋₇ acyl, C₁₋₆ alkoxycarbonyl, hydroxycarbonyl, aminocarbonyl optionally substituted by one or two C₁₋₆ alkyl groups, CF₃, C₁₋₆ alkyl substituted by C₁₋₆ alkoxy, C₁₋₆ alkylthio or by C₁₋₆ alkoxycarbonyl, or R₄ is phenyl or phenyl-C₁₋₄ alkyl optionally substituted in the phenyl ring by one or two of halogen, C₁₋₆ alkyl or C₁₋₆ alkoxy;     Z is a group of formula (a), (b) or (c) wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; and R₆ or R₇ is C₁₋₄ alkyl; having 5-HT₃ receptor antagonist activity, a process for their preparation and their use as pharmaceuticals.

  式 (I) 的化合物或其药学上可接受的盐： 其中 L 是 NH 或 O R₁ 是氢、氟或氯； R₂ 和 R₅ 独立地为氢或 C₁₋₆ 烷基，或合在一起为键；或 R₂ 和 R₃ 和/或 R₄ 和 R₅ 共同为 C₂₋₇ 聚亚甲基或-(CH₂)m-O-(CH₂)x-，其中 m 和 x 为 1 至 5，从而 m+x 为 2 至 6； R₄ 是 C₁₋₇酰基、C₁₋₆ 烷氧基羰基、羟基羰基、任选被一个或两个 C₁₋₆ 烷基取代的氨基羰基、CF₃、被 C₁₋₆ 烷氧基取代的 C₁₋₆ 烷基、或 R₄ 是苯基或苯基-C₁₋₄烷基，可任选在苯基环上被一个或两个卤素、C₁₋₆ 烷基或 C₁₋₆ 烷氧基取代； Z 是式(a)、(b)或(c)的基团 其中 n 是 2 或 3 p 是 1 或 2 q 是 1 至 3 r 为 1 至 3；以及 R₆ 或 R₇ 是 C₁₋₄烷基；具有 5-HT₃ 受体拮抗剂活性、其制备工艺和作为药物的用途。
• US4920127A
  申请人：——

  公开号：US4920127A

  公开（公告）日：1990-04-24