4-methoxy-2-phenylthiazole | 1516952-39-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-methoxy-2-phenylthiazole
• 英文别名: 2-(2-Phenylthiazol-4-yl) methanol；4-methoxy-2-phenyl-1,3-thiazole
• CAS: 1516952-39-8
• 化学式: C₁₀H₉NOS
• 分子量: 191.254
• InChiKey: XZAXAEZADFCYMR-UHFFFAOYSA-N

物化性质

• 沸点：
  320.5±34.0 °C(Predicted)
• 密度：
  1.184±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  50.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-溴吡啶 、 4-methoxy-2-phenylthiazole 在 palladium diacetate 、 potassium carbonate 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 0.17h， 以79%的产率得到4-methoxy-2-phenyl-5-(pyridin-3-yl)thiazole
  参考文献：
  名称：

  Synthesis of trisubstituted thiazoles by ligand-free palladium-catalyzed direct 5-arylation of 2,4-disubstituted thiazoles under conventional and microwave-assisted heating

  摘要：

  Trisubstituted thiazoles were synthesized with excellent yields using ligand-free, palladium-catalyzed, direct 5-arylation of 2,4-disubstituted thiazole and conventional or microwave-assisted heating. The palladium-catalyzed reaction yields were significantly influenced by LiCI additive, solvent, and heating method. The reaction times were reduced dramatically by employing microwave radiation instead of conventional heating. The synthetic methods can be applied to diverse 2,4,5-trisubstituted thiazoles by varying the aryl bromide and disubstituted thiazole reactants. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2013.10.053
• 作为产物：
  描述：

  溴乙酸甲酯 、 硫代苯甲酰胺 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 以50%的产率得到4-methoxy-2-phenylthiazole
  参考文献：
  名称：

  Synthesis of trisubstituted thiazoles by ligand-free palladium-catalyzed direct 5-arylation of 2,4-disubstituted thiazoles under conventional and microwave-assisted heating

  摘要：

  Trisubstituted thiazoles were synthesized with excellent yields using ligand-free, palladium-catalyzed, direct 5-arylation of 2,4-disubstituted thiazole and conventional or microwave-assisted heating. The palladium-catalyzed reaction yields were significantly influenced by LiCI additive, solvent, and heating method. The reaction times were reduced dramatically by employing microwave radiation instead of conventional heating. The synthetic methods can be applied to diverse 2,4,5-trisubstituted thiazoles by varying the aryl bromide and disubstituted thiazole reactants. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2013.10.053

文献信息

• Selective NPY (Y5) antagonists
  申请人：Marzabadi R. Mohammad

  公开号：US20050137240A1

  公开（公告）日：2005-06-23

  This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

  本发明涉及选择性拮抗NPY（Y5）受体的双环和三环化合物。本发明提供一种制药组合物，包括本发明化合物的治疗有效量和药学上可接受的载体。本发明提供了一种由本发明化合物的治疗有效量和药学上可接受的载体组合而成的制药组合物。本发明还提供了制备制药组合物的方法，包括将本发明化合物的治疗有效量和药学上可接受的载体组合。本发明进一步提供了使用本发明化合物制备用于治疗异常状态的制药组合物，其中减少人类Y5受体活性可缓解该异常状态。
• SELECTIVE NPY (Y5) ANTAGONISTS
  申请人：H. LUNDBECK A/S

  公开号：EP1194421B1

  公开（公告）日：2005-10-12
• EP1194421A4
  申请人：——

  公开号：EP1194421A4

  公开（公告）日：2002-09-11
• US6214853B1
  申请人：——

  公开号：US6214853B1

  公开（公告）日：2001-04-10
• US7273880B2
  申请人：——

  公开号：US7273880B2

  公开（公告）日：2007-09-25