2,4-二氟-N-甲氧基-N-甲基苯甲酰胺 | 198967-25-8

• 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: 2,4-二氟-N-甲氧基-N-甲基苯甲酰胺
• 英文名称: 2,4-difluoro-N-methoxy-N-methylbenzamide
• CAS: 198967-25-8
• 化学式: C₉H₉F₂NO₂
• mdl: MFCD02684298
• 分子量: 201.173
• InChiKey: UTSSEXHZQHZWED-UHFFFAOYSA-N

物化性质

• 沸点：
  305.6±32.0 °C(Predicted)
• 密度：
  1.261±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  29.5
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,4-二氟-N-甲氧基-N-甲基苯甲酰胺 在 硫酸 、 sodium hydride 作用下， 以 四氢呋喃 、 mineral oil 为溶剂， 反应 28.83h， 生成 6-(2,4-difluorophenyl)-4-hydroxy-5-methyl-2H-pyran-2-one
  参考文献：
  名称：

  WO2023/23242

  摘要：

  公开号：
• 作为产物：
  描述：

  二甲羟胺盐酸盐 、 2,4-二氟苯甲酰氯 在 吡啶 作用下， 以 氯仿 为溶剂， 反应 1.0h， 以89%的产率得到2,4-二氟-N-甲氧基-N-甲基苯甲酰胺
  参考文献：
  名称：

  Photochromic bi-naphthopyrans

  摘要：

  A series of novel 3-aryl-(3,3-diaryl-3H-naphtho[2,1-b]pyran-8-yl)-3H-naphtho[2,1-b]pyrans has been accessed from 6-bromo-2-naphthol via a four step transformation. Acylation of the dianion derived from the treatment of 6-bromo-2-naphthol with n-butyllithium with Weinreb amides and subsequent reaction with a 1,1,-diarylprop-2-yn-1-ol gave 8-aroyl-3H-naphtho[2,1-b]pyrans in good yield. Addition of lithium trimethylsilylacetylide to the foregoing 8-aroylnaphthopyrans proceeded smoothly with base-mediated desilyation to afford the target bi-naphthopyrans upon acid-catalysed reaction with 2-naphthol. Preliminary evaluation of the photochromic response of the new bi-naphthopyrans revealed reversible independent naphthopyran ring-opening leading to a complex photochromic signature. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.dyepig.2014.08.018

文献信息

• ALK5 INHIBITORS
  申请人：THERAVANCE BIOPHARMA R&D IP, LLC

  公开号：US20200188370A1

  公开（公告）日：2020-06-18

  The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

  本公开提供抑制活性素受体样激酶5（ALK5）的抑制剂。还公开了调节ALK5活性的方法以及治疗由ALK5介导的疾病的方法。
• Mo(CO)6 as a Solid CO Source in the Synthesis of Aryl/Heteroaryl Weinreb Amides under Microwave-Enhanced Condition
  作者：Raghu Ningegowda、Savitha Bhaskaran、Ayyiliath M. Sajith、Chandrashekar Aswathanarayanappa、M. Syed Ali Padusha、Nanjunda Swamy Shivananju、Babu Shubha Priya

  DOI：10.1071/ch16213

  日期：——

  The facile transformation of aryl/heteroaryl nonaflates into corresponding amides via Pd-catalyzed aminocarbonylation using Mo(CO)6 as a solid CO source under microwave-enhanced condition is reported. The method was found to be tolerant with respect to a diverse range of electronically biased aryl/heteroaryl nonaflates, and exceptional yields were obtained. The optimized protocol was further extended

  报道了在微波增强条件下，使用Mo（CO）6作为固体CO源，通过Pd催化的氨基羰基化，将芳基/杂芳基壬二酸芳酯轻松转化为相应的酰胺。发现该方法对于多种电子偏置的芳基/杂芳基壬二酸酯的耐受性，并且获得了优异的产率。优化的方案进一步扩展到多种胺。
• Therapeutic compounds
  申请人：——

  公开号：US20040229910A1

  公开（公告）日：2004-11-18

  The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

  本发明涉及某些新型苄基胺衍生物，其制备过程，含有它们的制药配方以及它们在医学治疗中的应用，特别是在抑郁症治疗中的应用。
• ALK5 inhibitors
  申请人：THERAVANCE BIOPHARMA R&D IP, LLC

  公开号：US10952996B2

  公开（公告）日：2021-03-23

  The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

  本公开提供了激活素受体样激酶5（ALK5）的抑制剂。还公开了调节 ALK5 活性的方法和治疗 ALK5 介导的疾病的方法。
• SUBSTITUTED BENZYLAMINES AND THEIR USE FOR THE TREATMENT OF DEPRESSION
  申请人：Akzo Nobel N.V.

  公开号：EP0898566B1

  公开（公告）日：2002-11-06