(2-乙基苯基)肼 | 19275-55-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (2-乙基苯基)肼
• 英文名称: (2-ethyl-phenyl)-hydrazine
• 英文别名: (2-Ethyl-phenyl)-hydrazin；(2-Ethylphenyl)hydrazine
• CAS: 19275-55-9
• 化学式: C₈H₁₂N₂
• mdl: MFCD02663066
• 分子量: 136.197
• InChiKey: JHPOWXCLWLEKBY-UHFFFAOYSA-N

物化性质

• 熔点：
  102.5-103 °C
• 沸点：
  247.7±19.0 °C(Predicted)
• 密度：
  1.056±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  38
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2-乙基苯基)肼 在 2-氯苯甲醛 作用下， 以 甲醇 、 乙醇 为溶剂， 反应 16.0h， 生成 4-(3-ethoxy-4-hydroxyphenyl)-1-(2-ethylphenyl)-1,4,5,7-tetrahydropyrazolo[3,4-b]pyridin-6-one
  参考文献：
  名称：

  [EN] COMPOUNDS, COMPOSITIONS AND METHODS USEFUL FOR CHOLESTEROL MOBILISATION
  [FR] COMPOSÉS, COMPOSITIONS ET MÉTHODES UTILES POUR LA MOBILISATION DU CHOLESTÉROL

  摘要：

  公开号：

  WO2012054535A3
• 作为产物：
  描述：

  2-ethylphenyl tosylate 在 bis[chloro(1,2,3-trihapto-allylbenzene)palladium(II)] 、 N-[2-二(1-金刚烷)磷苯基]吗啉 、 一水合肼 、 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 1.0h， 生成 (2-乙基苯基)肼
  参考文献：
  名称：

  Diversification of edaravone via palladium-catalyzed hydrazine cross-coupling: Applications against protein misfolding and oligomerization of beta-amyloid

  摘要：

  N-Aryl derivatives of edaravone were identified as potentially effective small molecule inhibitors of tau and beta-amyloid aggregation in the context of developing disease-modifying therapeutics for Alzheimer's disease (AD). Palladium-catalyzed hydrazine monoarylation protocols were then employed as an expedient means of preparing a focused library of 21 edaravone derivatives featuring varied N-aryl substitution, thereby enabling structure-activity relationship (SAR) studies. On the basis of data obtained from two functional biochemical assays examining the effect of edaravone derivatives on both fibril and oligomer formation, it was determined that derivatives featuring an N-biaryl motif were four-fold more potent than edaravone. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2015.11.022

文献信息

• Microwave-Promoted Solid-Acid-Catalyzed One-Pot Synthesis of Phthalazinones
  作者：Béla Török、Verona Outerbridge、Shainaz Landge、Hiroko Tamaki

  DOI：10.1055/s-0028-1088074

  日期：2009.6

  K-10 effectively catalyzed the condensation and substitution reactions. The approach was based on the direct cyclization of phthalaldehydic acid and opianic acid with substituted hydrazines. The reactions provided excellent yields and high selectivities in very short time (5-35 minutes). phthalazinones - phthalaldehydic acid - opianic acid - hydrazines - montmorillonite K-10 - microwave heating

  描述了一种一锅的固体酸催化的微波辅助的邻苯二氮酮合成。市售蒙脱土K-10有效催化了缩合和取代反应。该方法基于邻苯二酸和阿片酸与取代的肼的直接环化。反应在极短的时间内（5-35分钟）即可提供出色的收率和高选择性。 邻苯二酮-邻苯二酸-阿片酸-肼-蒙脱石K-10-微波加热
• Combined inorganic base promoted N-addition/[2,3]-sigmatropic rearrangement to construct homoallyl sulfur-containing pyrazolones
  作者：Shou-Jie Shen、Xiao-Li Du、Xiao-Li Xu、Yue-Hua Wu、Ming-gang Zhao、Jin-Yan Liang

  DOI：10.1039/c9ra07610g

  日期：——

  3]-sigmatropic rearrangement reaction of α-alkylidene pyrazolinones and propargyl sulfonium salts has been reported to construct homoallyl sulfur-containing pyrazolones with moderate to excellent yields. α-Alkylidene pyrazolinones function as N-nucleophilic agents distinguished from the reported C-addition reactions. Propargyl sulfonium salts were first involved in the [2,3]-sigmatropic rearrangement protocol

  据报道，第一个顺序组合的无机碱促进了α-亚烷基吡唑啉酮和炔丙基锍盐的N-加成/[2,3]-σ重排反应，以中等至优异的产率构建了高烯丙基含硫吡唑啉酮。 α-亚烷基吡唑啉酮作为 N-亲核试剂，与报道的 C-加成反应不同。炔丙基锍盐首先参与与成熟的成环反应不同的[2,3]-σ重排方案。优异的区域选择性、广泛的底物范围、克级合成和便捷的转化体现了该级联过程的合成优势。
• Continuous Flow Process For the Synthesis of Phenylhydrazine Salts and Substituted Phenylhydrazine Salts
  申请人：SHANGHAI HYBRID-CHEM TECHNOLOGIES

  公开号：US20190152896A1

  公开（公告）日：2019-05-23

  The present invention provided a continuous flow process for the synthesis of phenylhydrazine salts and substituted phenylhydrazine salts. Diazotization, reduction, acidic hydrolysis and salifying with acids are innovatively integrated together. Using acidic liquids of aniline or substituted aniline, diazotization reagents, reductants and acids as raw materials, phenylhydrazine derivative salts is obtained through the synthesis process, which is a three-step continuous tandem reaction including diazotization, reduction, acidic hydrolysis and salifying. The described synthesis process is a kind of integrated solutions, which is carried out in an integrated reactor. The feed inlets of the integrated reactor are continuously filled with raw materials. In the integrated reactor, diazotization, reduction, acidic hydrolysis and salifying are carried out continuously and orderly, and phenylhydrazine salts or substituted phenylhydrazine salts is obtained in the outlet of the integrated reactor without interruption. The total reaction time is no more than 20 min.

  本发明提供了一种连续流程，用于合成苯肼盐和取代苯肼盐。重氮化、还原、酸性水解和酸化与酸类创新地集成在一起。使用苯胺或取代苯胺的酸性液体、重氮化试剂、还原剂和酸类作为原料，通过合成过程获得苯肼衍生物盐，这是一个包括重氮化、还原、酸性水解和酸化的三步连续串联反应。所述的合成过程是一种集成解决方案，是在一个集成反应器中进行的。集成反应器的进料口连续填充原料。在集成反应器中，重氮化、还原、酸性水解和酸化被连续有序地进行，苯肼盐或取代苯肼盐在集成反应器的出口处获得，没有中断。总反应时间不超过20分钟。
• New pyrazolones as 11b-HSD1 inhibitors for diabetes
  申请人：Amrein Kurt

  公开号：US20070049574A1

  公开（公告）日：2007-03-01

  Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.

  公式化合物以及医药可接受的它们的盐和酯，其中R1至R4的意义如权利要求1中所给出，可以用作药物组合物。
• Synthesis and Antimicrobial Studies of Coumarin-Substituted Pyrazole Derivatives as Potent Anti-Staphylococcus aureus Agents
  作者：Rawan Alnufaie、Hansa Raj KC、Nickolas Alsup、Jedidiah Whitt、Steven Andrew Chambers、David Gilmore、Mohammad A. Alam

  DOI：10.3390/molecules25122758

  日期：——

  In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 µg/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed

  本文报道了 31 种新型香豆素取代吡唑衍生物的合成和抗菌研究。其中一些化合物已显示出对耐甲氧西林金黄色葡萄球菌 (MRSA) 的有效活性，最低抑菌浓度 (MIC) 低至 3.125 µg/mL。这些分子在抑制 MRSA 生物膜的发展和预先形成的生物膜的破坏方面同样有效。这些结果非常重要，因为 MRSA 菌株已成为人类最具威胁的病原体之一，并且这种细菌在死亡率方面正在绕过 HIV。