Benzamide, N-(1-naphthyl)-2-fluoro- | 198879-90-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: Benzamide, N-(1-naphthyl)-2-fluoro-
• 英文别名: 2-fluoro-N-naphthalen-1-ylbenzamide
• CAS: 198879-90-2
• 化学式: C₁₇H₁₂FNO
• 分子量: 265.287
• InChiKey: UFPUPMUMYWAQKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  20
• 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：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  Benzamide, N-(1-naphthyl)-2-fluoro- 在 dipotassium peroxodisulfate 、 sodium azide 、 四丁基溴化铵 、 copper diacetate 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 以72%的产率得到
  参考文献：
  名称：

  N-酰化的8-氨基喹啉通过远程CH-H活化的铜（II）催化直接叠氮化

  摘要：

  开发了一种简单有效的铜（II）通过远程CH活化N酰化的8-氨基喹啉的C5叠氮化的方法。在此反应的基础上，合成了一系列新的C5叠氮化的8-酰胺基喹啉，收率中等至良好。

  DOI：

  10.1002/cctc.201600874
• 作为产物：
  描述：

  1-萘胺 、 邻氟苯甲酰氯 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 生成 Benzamide, N-(1-naphthyl)-2-fluoro-
  参考文献：
  名称：

  A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors

  摘要：

  Distinct from previously reported urea and amide inhibitors of soluble epoxide hydrolase (sEH), a novel class of inhibitors were rationally designed based on the X-ray structure of this enzyme and known amide inhibitors. The structure-activity relationship (SAR) study was focused on improving the sEH inhibitory activity. Aminobenzisoxazoles emerged to be the optimal series, of which a potent human sEH inhibitor 7t was identified with a good pharmacokinetics (PK) profile. The strategy of employing aminoheterocycles as amide replacements may represent a general approach to develop mimics of known hydrolase or protease inhibitors containing an amide moiety. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.08.006

文献信息

• A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors
  作者：Hong C. Shen、Fa-Xiang Ding、Qiaolin Deng、Suoyu Xu、Xinchun Tong、Xiaoping Zhang、Yuli Chen、Gaochao Zhou、Lee-Yuh Pai、Magdalena Alonso-Galicia、Sophie Roy、Bei Zhang、James R. Tata、Joel P. Berger、Steven L. Colletti

  DOI：10.1016/j.bmcl.2009.08.006

  日期：2009.10

  Distinct from previously reported urea and amide inhibitors of soluble epoxide hydrolase (sEH), a novel class of inhibitors were rationally designed based on the X-ray structure of this enzyme and known amide inhibitors. The structure-activity relationship (SAR) study was focused on improving the sEH inhibitory activity. Aminobenzisoxazoles emerged to be the optimal series, of which a potent human sEH inhibitor 7t was identified with a good pharmacokinetics (PK) profile. The strategy of employing aminoheterocycles as amide replacements may represent a general approach to develop mimics of known hydrolase or protease inhibitors containing an amide moiety. (C) 2009 Elsevier Ltd. All rights reserved.
• Copper(II)-Catalyzed Direct Azidation of<i>N</i>-Acylated 8-Aminoquinolines by Remote C−H Activation
  作者：Yandong Dou、Zhenda Xie、Zongguo Sun、Hongli Fang、Chao Shen、Pengfei Zhang、Qing Zhu

  DOI：10.1002/cctc.201600874

  日期：2016.12.7

  A simple and efficient copper(II)‐catalyzed C5 azidation of N‐acylated 8‐aminoquinolines by remote C−H activation was developed. On the basis of this reaction, a series of new C5‐azidated 8‐amidequinolines were synthesized in moderate to good yields.

  开发了一种简单有效的铜（II）通过远程CH活化N酰化的8-氨基喹啉的C5叠氮化的方法。在此反应的基础上，合成了一系列新的C5叠氮化的8-酰胺基喹啉，收率中等至良好。