2-(4-Methylphenoxy)-3,5-dichlorpyridin | 28232-17-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(4-Methylphenoxy)-3,5-dichlorpyridin
• 英文别名: 3,5-Dichloro-2-(4-methylphenoxy)pyridine
• CAS: 28232-17-9
• 化学式: C₁₂H₉Cl₂NO
• 分子量: 254.116
• InChiKey: VXFVLSFEUCYWEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  22.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2,3,5-三氯吡啶 、 对甲酚 在 copper(l) iodide 、 四甲基乙二胺 、 caesium carbonate 作用下， 以 二甲基亚砜 为溶剂， 反应 24.0h， 以93%的产率得到2-(4-Methylphenoxy)-3,5-dichlorpyridin
  参考文献：
  名称：

  Copper-catalyzed highly regioselective 2-aryloxylation of 2,x-dihalopyridines

  摘要：

  2,x-Dihalopyridines reacted with phenols catalyzed by CuI/TMEDA in the presence of Cs2CO3 in DMSO at 110 degrees C under nitrogen atmosphere for 24 h to afford 2-aryloxypyridines in good to high yields except p-nitrophenol. To expand this methodology, a vanilloid receptor ligand used in treatments was prepared in good yield. This method has potential utility in the synthesis of pharmaceuticals, agrochemicals and even natural products. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2012.10.025

文献信息

• [EN] GLYCINE B ANTAGONISTS<br/>[FR] ANTAGONISTES DE LA GLYCINE B
  申请人：MERZ PHARMA GMBH & CO KGAA

  公开号：WO2010037533A1

  公开（公告）日：2010-04-08

  The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.

  该发明涉及喹啉衍生物及其药用盐。该发明还涉及一种制备这种化合物的方法。该发明的化合物是甘氨酸B拮抗剂，因此对于控制和预防各种疾病，包括神经系统疾病，非常有用。
• GLYCINE B ANTAGONIST
  申请人：Henrich Markus

  公开号：US20110190342A1

  公开（公告）日：2011-08-04

  The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.

  本发明涉及喹啉衍生物及其药学上可接受的盐。本发明还涉及制备这种化合物的过程。本发明的化合物是甘氨酸B拮抗剂，因此对控制和预防各种疾病，包括神经系统疾病，非常有用。
• US8288549B2
  申请人：——

  公开号：US8288549B2

  公开（公告）日：2012-10-16
• Copper-catalyzed highly regioselective 2-aryloxylation of 2,x-dihalopyridines
  作者：Qizhong Zhou、Bin Zhang、Tieqi Du、Haining Gu、Yuyuan Ye、Huajiang Jiang、Rener Chen

  DOI：10.1016/j.tet.2012.10.025

  日期：2013.1

  2,x-Dihalopyridines reacted with phenols catalyzed by CuI/TMEDA in the presence of Cs2CO3 in DMSO at 110 degrees C under nitrogen atmosphere for 24 h to afford 2-aryloxypyridines in good to high yields except p-nitrophenol. To expand this methodology, a vanilloid receptor ligand used in treatments was prepared in good yield. This method has potential utility in the synthesis of pharmaceuticals, agrochemicals and even natural products. (C) 2012 Elsevier Ltd. All rights reserved.