N-hydroxy-N-(2-methoxyphenyl)acetamide | 82344-33-0

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-hydroxy-N-(2-methoxyphenyl)acetamide
• 英文别名: N-acetyl-2-methoxyphenylhydroxylamine；N-acetyl-N-(2-methoxyphenyl)hydroxylamine
• CAS: 82344-33-0
• 化学式: C₉H₁₁NO₃
• 分子量: 181.191
• InChiKey: DJMUQORMZAYKFI-UHFFFAOYSA-N

物化性质

• 沸点：
  315.2±44.0 °C(Predicted)
• 密度：
  1.240±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-hydroxy-N-(2-methoxyphenyl)acetamide 在 氯化亚砜 作用下， 以 乙醚 为溶剂， 反应 1.0h， 以84%的产率得到N-aceto-2-chloro-6-methoxyaniline
  参考文献：
  名称：

  Ayyangar, N. R.; Kalkote, U. R.; Nikrad, P. V., Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1983, vol. 22, # 9, p. 872 - 877

  摘要：

  DOI：
• 作为产物：
  描述：

  2-硝基苯甲醚 、 alkaline earth salt of/the/ methylsulfuric acid 在 氯化铵 、 锌 作用下， 以37.9%的产率得到N-hydroxy-N-(2-methoxyphenyl)acetamide
  参考文献：
  名称：

  Rhodium(III)-catalyzed internal oxidative coupling of N-hydroxyanilides with alkenes via C–H activation

  摘要：

  Described herein is an efficient new method for ortho-olefination of anilides in the presence of AgSbF6 and NaOAc via rhodium(III)-catalyzed internal oxidative C-H bond activation based on hydroxyl as directing and oxidative group. A range of alkenes and functional groups on acetanilides is supported and a possible mechanism is proposed according to the experimental results. (C) 2015 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2015.07.070

文献信息

• 一种4-氟取代芳基胺类化合物及其合成方法
  申请人：江苏笃行致远新材料科技有限公司

  公开号：CN113416139B

  公开（公告）日：2022-06-03

  本发明公开了一种4‑氟取代芳基胺类化合物的合成方法，包括以下步骤：1)以酰基保护的苯基羟胺为底物，在极性溶剂中，以磺酰氟为氟源，在碱性条件下生成4‑氟取代苯胺类化合物；2)在稀酸性条件下或者Pd催化氢化进行脱保护基团，得到所述4‑氟取代芳基胺类化合物。本发明合成的4‑氟取代的苯胺类化合物，由于氟原子引入极大程度上增加其亲脂性，因此能广泛用于含氟药物、农药以及染料中间体的制备；同时，本发明采用的原料均为工业化产品，价廉易得，具有市售；通过本发明制得的4‑氟芳基苯胺收率高，能够以大于90％的收率得到纯度≥99％的产物；本发明操作简单，成本低廉的工艺十分适用于工业化，能够广泛推广使用。
• NOVEL INDOLE DERIVATIVE HAVING, CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP
  申请人：Kawashima Kenji

  公开号：US20110124668A1

  公开（公告）日：2011-05-26

  The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKKβ inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKKβ. In the formula, R 1 represents a hydrogen atom, a lower alkyl group which may have a substituent, a hydroxy group, or a lower alkoxy group which may have a substituent, or the like; R 2 represents a hydrogen atom, a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, or a heterocyclic group which may have a substituent, or the like; R 3 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group which may have a substituent, a lower alkynyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, or the like; m represents 0, 1, 2, or the like.

  本发明涉及具有氨基甲酰基、尿素基和取代氧基或其盐的新型吲哚衍生物的合成研究以及其药理作用。通式（1）表示的化合物及其盐具有IKKβ抑制活性，并可用作预防和/或治疗与IKKβ相关的疾病的药物。在该式中，R1表示氢原子、可能具有取代基的较低烷基、羟基或可能具有取代基的较低烷氧基等；R2表示氢原子、可能具有取代基的较低烷基、可能具有取代基的较低环烷基、可能具有取代基的芳基或可能具有取代基的杂环基等；R3表示卤素原子、可能具有取代基的较低烷基、可能具有取代基的较低烯基、可能具有取代基的较低炔基、可能具有取代基的较低环烷基、可能具有取代基的芳基、可能具有取代基的杂环基等；m表示0、1、2或类似物。
• NOVEL INDOLE DERIVATIVE HAVING CARBAMOYL GROUP, UREIDE GROUP AND SUBSTITUTED OXY GROUP
  申请人：Santen Pharmaceutical Co., Ltd

  公开号：EP2314575A1

  公开（公告）日：2011-04-27

  The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IRKβ inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKKβ. In the formula, R1 represents a hydrogen atom, a lower alkyl group which may have a substituent, a hydroxy group, or a lower alkoxy group which may have a substituent, or the like; R2 represents a hydrogen atom, a lower alkyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, or a heterocyclic group which may have a substituent, or the like; R3 represents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group which may have a substituent, a lower alkynyl group which may have a substituent, a lower cycloalkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, or the like; m represents 0, 1, 2, or the like.

  本发明涉及具有氨基甲酰基、脲基和取代氧基的新型吲哚衍生物或其盐的合成研究，以及这些衍生物的药物作用。通式（1）代表的化合物及其盐具有 IRKβ 抑制活性，可作为预防和/或治疗被认为与 IKKβ 有关的疾病的药物。式中，R1 代表氢原子、可能具有取代基的低级烷基、羟基或可能具有取代基的低级烷氧基等；R2 代表氢原子、可能具有取代基的低级烷基、可能具有取代基的低级环烷基、可能具有取代基的芳基或可能具有取代基的杂环基等；R3 代表卤素原子、可具有取代基的低级烷基、可具有取代基的低级烯基、可具有取代基的低级炔基、可具有取代基的低级环烷基、可具有取代基的芳基、可具有取代基的杂环基等；m 代表 0、1、2 或类似物。
• NOVEL INDOLE DERIVATIVE HAVING CARBAMOYL GROUP, UREIDO GROUP AND SUBSTITUTED OXY GROUP
  申请人：Santen Pharmaceutical Co., Ltd

  公开号：EP2314575B1

  公开（公告）日：2013-06-19
• Novel orthohalogenation reaction. Synthesis of orthochloroarylamines from nitroarenes.
  作者：Nagaraj R. Ayyangar、Uttam R. Kalkote、Pandurang V. Nikrad

  DOI：10.1016/s0040-4039(00)87031-8

  日期：1982.1