N-(2-methoxyphenyl)benzimidoyl chloride | 59386-96-8

• 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: N-(2-methoxyphenyl)benzimidoyl chloride
• 英文别名: Benzoesaeure-<2-methoxy-phenylimid>-chlorid；N-(2-methoxyphenyl)benzenecarboximidoyl chloride
• CAS: 59386-96-8
• 化学式: C₁₄H₁₂ClNO
• 分子量: 245.708
• InChiKey: KLYMEZRMPXETGC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  21.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(2-methoxyphenyl)benzimidoyl chloride 在 sodium ethanolate 作用下， 以 乙醚 、 乙醇 为溶剂， 生成 N-<2-Methoxy-phenyl>-N-<3-methoxycarbonyl-phenyl>-benzamid
  参考文献：
  名称：

  Messer,M.; Farge,D., Bulletin de la Societe Chimique de France, 1968, p. 2832 - 2842

  摘要：

  DOI：
• 作为产物：
  描述：

  N-(2-甲氧基苯基)苯甲酰胺 在 氯化亚砜 作用下， 反应 10.0h， 生成 N-(2-methoxyphenyl)benzimidoyl chloride
  参考文献：
  名称：

  氧化银（II）介导的2,4-二芳基喹唑啉的合成

  摘要：

  描述了合成2，4-二芳基喹唑啉的单釜法，该法涉及氧化银介导的C H活化/ C N键形成过程。提出了有关取代基效应的通用方法以及导致工艺优化的研究。机理研究为自由基中间体参与反应过程提供了支持。

  DOI：

  10.1016/j.tetlet.2018.05.019

文献信息

• Silver(II) oxide-mediated synthesis of 2,4-diarylquinazolines
  作者：Wing Cheung、Raymond J. Patch、Mark R. Player

  DOI：10.1016/j.tetlet.2018.05.019

  日期：2018.6

  4-diarylquinazolines is described which involves a silver oxide-mediated CH activation/CN bond formation process. The generality of this method with respect to substituent effects is presented along with studies leading to process optimization. Mechanistic investigations provide support for the involvement of radical intermediates in the reaction process.

  描述了合成2，4-二芳基喹唑啉的单釜法，该法涉及氧化银介导的C H活化/ C N键形成过程。提出了有关取代基效应的通用方法以及导致工艺优化的研究。机理研究为自由基中间体参与反应过程提供了支持。
• Potential antitumor agents. 40. Orally active 4,5-disubstituted derivatives of amsacrine
  作者：William A. Denny、Graham J. Atwell、Bruce C. Baguley

  DOI：10.1021/jm00369a021

  日期：1984.3

  5-disubstituted derivatives all showed high activity when administered ip against ip-implanted P-388, but activity varied widely when the compounds were given orally. 4-Methoxy and 4-carbamoyl derivatives proved essentially inactive, whereas 4-methyl and 4-methylcarbamoyl derivatives retained activity. Exceptional oral activity was shown by the 4-methyl-5-methylcarbamoyl derivative, making this amsacrine

  DNA嵌入剂amsacrine是治疗人类白血病和淋巴瘤的有效药物，但实体瘤活性极低。作为鉴定具有更广谱活性的类似物的第一步，对通过口服（po）和腹膜内（ip）途径给予的Amsacrine类似物的体内抗白血病（P-388）活性进行了比较。一系列的4-取代和4,5-二取代的衍生物在ip注射时对ip植入的P-388均显示出高活性，但是当口服给予化合物时，活性变化很大。事实证明4-甲氧基和4-氨基甲酰基衍生物基本上没有活性，而4-甲基和4-甲基氨基甲酰基衍生物保持活性。4-甲基-5-甲基氨基甲酰基衍生物显示出非凡的口服活性，使该氨溴萘衍生物值得进一步测试。
• Chemistry and hypoglycemic activity of benzimidoylpyrazoles
  作者：James R. Shroff、Victor Bandurco、Rohit Desai、Sidney Kobrin、Peter Cervoni

  DOI：10.1021/jm00144a031

  日期：1981.12

  (tolazamide, phenformin, and buformin) in several experimental models show that these compounds seem to combine in one molecule some of the biological activities of the beta-cytotrophic sulfonylureas and some of the activities of the biguanides. A synthetic scheme for the preparation of the benzimidolypyrazoles and a preliminary structure-activity relationship are presented.

  合成了一系列苯并亚氨基酰基吡唑类，并作为降血糖药进行了评估。1-（N-环己基苯并亚甲基）-5-甲基-3-吡唑甲酸甲酯（13）和1- [N-（4-甲氧基苯基）苯并亚甲基] -5-甲基-3-吡唑甲酸甲酯（33）是其中两个更有趣的化合物。在几个实验模型中将这些苯甲亚氨基酰基吡唑类与经典标准品（甲苯磺酰胺，苯乙双胍和丁二甲酰胺）进行比较，结果表明，这些化合物似乎在一个分子中结合了β-细胞营养性磺酰脲类的某些生物活性和双胍类的某些活性。提出了合成苯甲酰亚胺基吡唑的合成方案，并初步建立了结构-活性关系。
• 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.
• Fabian et al., Bulletin de la Societe Chimique de France, 1956, p. 287,291
  作者：Fabian et al.

  DOI：——

  日期：——