(E/Z)-N-phenyl-1-naphthimidoyl chloride | 872798-01-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: (E/Z)-N-phenyl-1-naphthimidoyl chloride
• 英文别名: N-phenyl-1-naphthylacetimidoyl chloride；N-phenyl-[1]naphthimidoyl chloride；N-phenylnaphthalene-1-carboximidoyl chloride
• CAS: 872798-01-1
• 化学式: C₁₇H₁₂ClN
• 分子量: 265.742
• InChiKey: VUMDSYVRKZSOSY-UHFFFAOYSA-N

物化性质

• 沸点：
  422.3±28.0 °C(Predicted)
• 密度：
  1.13±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  12.4
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (E/Z)-N-phenyl-1-naphthimidoyl chloride 在 氯仿 、 paraffin 作用下， 生成 4(1H)-喹啉酮,2-(1-萘基)-
  参考文献：
  名称：

  Staskun, Journal of the South African Chemical Institute, 1956, vol. 9, p. 89

  摘要：

  DOI：
• 作为产物：
  描述：

  苯胺 在 五氯化磷 、 三乙胺 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 反应 22.0h， 生成 (E/Z)-N-phenyl-1-naphthimidoyl chloride
  参考文献：
  名称：

  [EN] TRIAZINE MEDIATED LIVING RADICAL CONTROLLED POLYMERIZATION
  [FR] POLYMÉRISATION RADICALAIRE CONTRÔLÉE VIVANTE MÉDIÉE PAR UNE TRIAZINE

  摘要：

  该披露提供了模块化的三嗪基单分子引发剂化合物，可用于乙烯类单体的受控自由基聚合。

  公开号：

  WO2015061189A1

文献信息

• Accessing indole–isoindole derivatives <i>via</i> palladium-catalyzed [3+2] cyclization of isocyanides with alkynyl imines
  作者：Dianpeng Chen、Jianming Li、Gongle Liu、Xiuhua Zhang、Xin Wang、Yongwei Liu、Xuan Liu、Xinghai Liu、Yongqin Li、Yingying Shan

  DOI：10.1039/d3cc02654j

  日期：——

  proceeds via a palladium-catalyzed [3+2] cyclization of isocyanides with alkynyl imines. In this transformation, the palladium catalyst has a triple role, serving simultaneously as a π acid, a transition-metal catalyst and a hydride ion donor, thus enabling the dual function of isocyanide both as a C1 synthon for cyanation and a C1N1 synthon for imidoylation. Significantly, the reaction is the sole successful

  开发了一种制备吲哚-异吲哚衍生物的简便方案，并通过钯催化的异氰化物与炔基亚胺的[3+2]环化进行。在此转化中，钯催化剂具有三重作用，同时充当π酸、过渡金属催化剂和氢负离子供体，从而使异氰化物具有双重功能，即作为氰化的C1合成子和用于亚氨酰化的C1N1合成子。值得注意的是，该反应是获得吲哚-异吲哚衍生物的唯一成功范例，并将为组装独特的N-杂环框架开辟新途径。此外，该方案的合成价值在生理活性分子的后期修饰和聚集诱导发射化合物的构建中得到了证明。
• 5-Imino-1,2,4-Thiadiazoles: First Small Molecules As Substrate Competitive Inhibitors of Glycogen Synthase Kinase 3
  作者：Valle Palomo、Daniel I. Perez、Concepcion Perez、Jose A. Morales-Garcia、Ignacio Soteras、Sandra Alonso-Gil、Arantxa Encinas、Ana Castro、Nuria E. Campillo、Ana Perez-Castillo、Carmen Gil、Ana Martinez

  DOI：10.1021/jm201463v

  日期：2012.2.23

  Cumulative evidence strongly supports that glycogen synthase kinase-3 (GSK-3) is a pathogenic molecule when it is up-dysregulated, emerging as an important therapeutic target in severe unmet human diseases. GSK-3 specific inhibitors might be promising effective drugs for the treatment of devastating pathologies such as neurodegenerative diseases, stroke, and mood disorders. As GSK-3 has the ability to phosphorylate primed substrates, small molecules able to bind to this site should be perfect drug candidates, able to partially block the activity of the enzyme over some specific substrates. Here, we report substituted 5-imino-1,2,4-thiadiazoles as the first small molecules able to inhibit GSK-3 in a substrate competitive manner. These compounds are cell permeable, able to decrease inflammatory activation and to selectively differentiate neural stem cells. Overall, 5-imino-1,2,4-thiadiazoles are presented here as new molecules able to decrease neuronal cell death and to increase endogenous neurogenesis blocking the GSK-3 substrate site
• Transition Metal-Free Visible Light-Driven Photoredox Oxidative Annulation of Arylamidines
  作者：Zi-chao Shen、Pan Yang、Yu Tang

  DOI：10.1021/acs.joc.5b02366

  日期：2016.1.4

  A fast catalytic synthesis of multisubstituted quinazolines from readily available amidines via visible light-mediated oxidative C(sp(3))-C(sp(2)) bond formation has been established. This reaction is a metal-free oxidative coupling catalyzed by a photoredox organocatalyst. The protocol features low catalyst loading (1 mol %).
• Solvent/Oxidant-Switchable Synthesis of Multisubstituted Quinazolines and Benzimidazoles via Metal-Free Selective Oxidative Annulation of Arylamidines
  作者：Jian-Ping Lin、Feng-Hua Zhang、Ya-Qiu Long

  DOI：10.1021/ol500864r

  日期：2014.6.6

  A fast and simple divergent synthesis of multisubstituted quinazolines and benzimidazoles was developed from readily available amidines, via iodine(III)-promoted oxidative C(sp(3))-C(sp(2)) and C(sp(2))-N bond formation in nonpolar and polar solvents, respectively. Further selective synthesis of quinazolines in polar solvent was realized by TEMPO-catalyzed sp(3)C-H/sp(2)C-H direct coupling of the amidine with K2S2O8 as the oxidant. No metal, base, or other additives were needed.
• Familial Aggregation of 7-Year Changes in Musculoskeletal Fitness
  作者：P. T. Katzmarzyk、N. Gledhill、L. Perusse、C. Bouchard

  DOI：10.1093/gerona/56.12.b497

  日期：2001.12.1

  The purpose of this study was to determine the degree of familial resemblance in baseline and 7-year changes in musculoskeletal fitness. Data front the 1981 Canada Fitness Survey and the Campbell's Survey 7-year follow-up were used. The sample consisted of 1264 people (635 males and 629 females) between the ages of 7 and 69 years for whom measurements of musculoskeletal fitness were available at baseline. A subsample of 834 people had measurements at both baseline and 7-year follow-up. Sit-and-reach trunk flexibility, number of push-ups without time limit, number of sit-ups in 60 seconds, and hand-grip strength were used as indicators of musculoskeletal fitness. The data were adjusted for the effects of age and body mass index (and baseline level of the variable for changes) by using regression procedures, and they were standardized to zero mean and unit variance within each of the four sex-by-generation groups (fathers, mothers, sons, and daughters), Familial correlation models were fitted to the data by using the computer software SEGPATH. The results indicate significant familial resemblance for all indicators of musculoskeletal fitness for baseline measures and 7-year changes. The heritabilities, or the percentages of the total variance attributable to heredity, were 64% for trunk flexibility, 37% for push-ups, 59% for sit-ups, and 48% for grip strength. Similarly, heritabilities for the change scores were 48% for trunk flexibility, 52% for push-ups, 41% for sit-ups, and 32% for grip strength. The results suggest that familial, and perhaps genetic, factors are important in explaining the variance in musculoskeletal fitness not only cross-sectionally but also for changes over time.