2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine | 1167570-71-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
• CAS: 1167570-71-9
• 化学式: C₉H₇F₃N₂
• 分子量: 200.163
• InChiKey: VQIVZKZJGBXQIR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  17.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine 、 3-碘苯酚 在 palladium diacetate 、 三苯基膦 caesium carbonate 作用下， 以 1,4-二氧六环 为溶剂， 以78%的产率得到3-(2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl)phenol
  参考文献：
  名称：

  [EN] IMIDAZO [1,2-A] PYRIDINE COMPOUNDS
  [FR] COMPOSÉS D'IMIDAZO[1,2-A]PYRIDINE

  摘要：

  公开号：

  WO2009086123A8
• 作为产物：
  描述：

  一氯丙酮 、 2-氨基-3-三氟甲基吡啶 在 sodium iodide 碳酸氢钠 作用下， 以 乙醇 为溶剂， 以51%的产率得到2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
  参考文献：
  名称：

  [EN] IMIDAZO [1,2-A] PYRIDINE COMPOUNDS
  [FR] COMPOSÉS D'IMIDAZO[1,2-A]PYRIDINE

  摘要：

  公开号：

  WO2009086123A8

文献信息

• Imidazo [1,2-A] Pyridine Compounds
  申请人：Singhaus, JR. Robert Ray

  公开号：US20110112135A1

  公开（公告）日：2011-05-12

  This invention relates generally to imidazo[1,2-a]pyridine-based modulators of Liver X receptors (LXRs) having formula (I) and related methods: wherein R 2 is C 6 -C 10 aryl or heteroaryl including 5-10 atoms, each of which is: (i) substituted with 1 R 7 , and (ii) optionally substituted with from 1-5 R e ; and R 1 , R 3 , R 4 , R 5 , R 6 , R 7 , and R e are defined herein.

  本发明涉及一般的imidazo[1,2-a]吡啶基LXR（肝X受体）调节剂，其具有公式（I）和相关方法：其中R2是C6-C10芳基或杂环芳基，包括5-10个原子，每个原子：（i）被1个R7取代，（ii）可选地被1-5个Re取代；R1、R3、R4、R5、R6、R7和Re在此定义。
• 3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists
  作者：Robert R. Singhaus、Ronald C. Bernotas、Robert Steffan、Edward Matelan、Elaine Quinet、Ponnal Nambi、Irene Feingold、Christine Huselton、Anna Wilhelmsson、Annika Goos-Nilsson、Jay Wrobel

  DOI：10.1016/j.bmcl.2009.11.098

  日期：2010.1

  Replacement of a quinoline with an imidazo[1,2-a]pyridine in a series of liver X receptor (LXR) agonists incorporating a [3-(sulfonyl)aryloxyphenyl] side chain provided high affinity LXR ligands 7. In functional assays of LXR activity, good agonist potency and efficacy were found for several analogs. (C) 2009 Elsevier Ltd. All rights reserved.
• IMIDAZO [1,2-A] PYRIDINE COMPOUNDS
  申请人：Wyeth LLC

  公开号：EP2231660A1

  公开（公告）日：2010-09-29
• TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20170305902A1

  公开（公告）日：2017-10-26

  The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , L, X 1 , X 2 , and X 3 , are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
• [EN] TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE<br/>[FR] DERIVES DE TETRAHYDRONAPHTYRIDINE EN TANT QUE MODULATEURS ALLOSTERIQUES NEGATIFS DE MGLUR2, COMPOSITIONS ET UTILISATION DE CEUX-CI
  申请人：MERCK SHARP & DOHME

  公开号：WO2016032921A1

  公开（公告）日：2016-03-03

  The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.