5-bromo-2-(4-methoxyphenoxy)pyridine | 1249814-92-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-bromo-2-(4-methoxyphenoxy)pyridine
• 英文别名: 5-bromo-(4-methoxyphenoxy)pyridine
• CAS: 1249814-92-3
• 化学式: C₁₂H₁₀BrNO₂
• 分子量: 280.121
• InChiKey: YCNCBGFMDCPOEY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  31.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2,5-二溴吡啶 、 4-甲氧基苯酚 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95%的产率得到5-bromo-2-(4-methoxyphenoxy)pyridine
  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

• PARTIALLY SATURATED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
  申请人：TAISHO PHARMACEUTICAL CO., LTD

  公开号：US20150175541A1

  公开（公告）日：2015-06-25

  There are provided compounds having a superior PHD2 inhibitory effect that are represented by general formula (I′): (in the above-mentioned general formula (I′), W, Y, R 2 , R 3 , R 4 , and Y 4 are as described hereinabove), or pharmaceutically acceptable salts thereof.

  提供了一些化合物，具有优越的PHD2抑制作用，其通式表示为(I'):(在上述通式(I')中，W、Y、R2、R3、R4和Y4如上所述)，或其药学上可接受的盐。
• SELECTIVE BRUTON'S TYROSINE KINASE INHIBITOR AND USE THEREOF
  申请人：Hangzhou Hertz Pharmaceutical Co., Ltd.

  公开号：EP3543239A1

  公开（公告）日：2019-09-25

  The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug for treating diseases, disorders or conditions benefiting from the inhibition of Bruton's tyrosine kinase activity. The compound of the present invention has anti-proliferation and inhibitory effects on tumor cell strains such as A549, MINO, OCI-LY10 and TMD-8, and shows an excellent anti-tumor activity in tumor models such as Mino subcutaneous xenografts, and can be applied in drugs for treating solid tumors or leukemia associated with cell proliferation in humans or animals. The compound of the present invention has good pharmacokinetic properties, and can be applied to the oral treatment of solid tumors or leukemia associated with the cell proliferation in humans or animals or autoimmune diseases. The compound of the present invention has the property of a low hERG channel blockade.

  本发明涉及一种选择性布鲁顿酪氨酸激酶（BTK）抑制剂化合物、药物组合物、制剂及其在制备用于治疗受益于抑制布鲁顿酪氨酸激酶活性的疾病、失调或病症的药物中的用途。本发明化合物对A549、MINO、OCI-LY10和TMD-8等肿瘤细胞株具有抗增殖和抑制作用，在Mino皮下异种移植等肿瘤模型中显示出优异的抗肿瘤活性，可应用于治疗与人或动物细胞增殖相关的实体瘤或白血病的药物中。本发明的化合物具有良好的药代动力学特性，可应用于与人或动物细胞增殖相关的实体瘤或白血病或自身免疫性疾病的口服治疗。本发明化合物具有低 hERG 通道阻断特性。
• Selective Bruton's tyrosine kinase inhibitor and use thereof
  申请人：HANGZHOU HERTZ PHARMACEUTICAL CO., LTD.

  公开号：US10711006B2

  公开（公告）日：2020-07-14

  The present invention relates to a selective Bruton's tyrosine kinase (BTK) inhibitor compound, a pharmaceutical composition, preparation and use thereof in preparation of a drug. The compound of the present invention has a structure of Formula II or Formula II′: or their optical isomers, or pharmaceutically acceptable salts or solvates; where each Rg is independently H, halogen, —CF2H, —CF3, —CN, C1-C3 alkyl, or C1-C3 alkoxy; n is selected from 0, 1 and 2; Rd is selected from Re is selected from H, CH3, C2-C6 alkyl, C1-C6 azaalkyl, and C1-C6 oxaalkyl, wherein CH3, C2-C6 alkyl, C1-C6 azaalkyl and C1-C6 oxaalkyl are further substituted with amino, hydroxyl, and C1-C3 alkyl; Y1, Y2, Y3 and Y4 are independently selected from C(Rf) and N, and at least one of Y1, Y2, Y3 and Y4 is N, wherein Rf is selected from H, halogen, C1-C3 alkyl, —CF3, and —CF2H.

  本发明涉及一种选择性布鲁顿酪氨酸激酶(BTK)抑制剂化合物、包含该化合物的药物组合物及其制备和在制备药物中的用途。本发明的化合物具有式II或式II'的结构： 或其光学异构体，或药学上可接受的盐或溶剂合物； 其中，每个Rg独立地选自H、卤素、—CF2H、—CF3、—CN、C1-C3烷基或C1-C3烷氧基； n选自0、1和2； Rd选自 Re选自H、CH3、C2-C6烷基、C1-C6氨基烷基和C1-C6氧基烷基，其中 、C2-C6烷基、C1-C6氨基烷基和C1-C6氧基烷基进一步被氨基、羟基和C1-C3烷基取代； Y1、Y2、Y3和Y4独立地选自C(Rf)和N，且Y1、Y2、Y3和Y4中至少有一个为N，其中Rf选自H、卤素、C1-C3烷基、— 和—CF2H。
• US9422240B2
  申请人：——

  公开号：US9422240B2

  公开（公告）日：2016-08-23