2-fluoro-4-[4-(4-fluorophenyl)-1,3-thiazol-5-yl]pyridine | 742078-83-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-fluoro-4-[4-(4-fluorophenyl)-1,3-thiazol-5-yl]pyridine
• 英文别名: 4-[4-(4-fluorophenyl) thiazol-5-yl]-2-fluoropyridine；4-(4-fluorophenyl)-5-(2-fluoropyridin-4-yl)-1,3-thiazole
• CAS: 742078-83-7
• 化学式: C₁₄H₈F₂N₂S
• 分子量: 274.294
• InChiKey: ZIPUZFCUIIEWNF-UHFFFAOYSA-N

物化性质

• 沸点：
  379.6±37.0 °C(predicted)
• 密度：
  1.342±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-fluoro-4-[4-(4-fluorophenyl)-1,3-thiazol-5-yl]pyridine 在 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 生成 4-{4-(4-Fluoro-phenyl)-5-[2-((S)-1-phenyl-ethylamino)-pyridin-4-yl]-thiazol-2-yl}-1-methyl-piperidin-4-ol
  参考文献：
  名称：

  Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis

  摘要：

  A library of trisubstituted oxazoles, thiazoles, imidazoles (1,2,4- and 2,4,5-substituted) and imidazo[1,2-b]pyridines was prepared and evaluated in vitro as p38alpha inhibitors and in vivo in several models of rheumatoid arthritis. Four structures 32, 37, 45 and 59-were identified as potent inhibitors of p38alpha with high efficacy in the LPS induced TNFalpha release model in the mouse, the adjuvant induced arthritis and the collagen induced arthritis in the rat with ED(50)s between 1.0 and 9.5 mg/kg p.o. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.03.106
• 作为产物：
  描述：

  1-(4-氟苯基)-2-(2-氟吡啶-4-基)乙酮 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 四氢呋喃 、 DMF (N,N-dimethyl-formamide) 为溶剂， 反应 7.33h， 生成 2-fluoro-4-[4-(4-fluorophenyl)-1,3-thiazol-5-yl]pyridine
  参考文献：
  名称：

  [EN] TETRACYCLIC INHIBITORS OF JANUS KINASES
  [FR] INHIBITEURS TETRACYCLIQUES DE JANUS KINASES

  摘要：

  本发明提供了能调节雅努斯激酶活性并且在治疗与雅努斯激酶活性相关的疾病方面有用的化合物，例如免疫相关疾病和癌症。

  公开号：

  WO2005105814A1

文献信息

• Tetracyclic inhibitors of Janus kinases
  申请人：Rodgers D. James

  公开号：US20060106020A1

  公开（公告）日：2006-05-18

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了一种调节Janus激酶活性的化合物，可用于治疗与Janus激酶活性相关的疾病，例如免疫相关疾病和癌症。
• TETRACYCLIC INHIBITORS OF JANUS KINASES
  申请人：Rodgers James D.

  公开号：US20090215766A1

  公开（公告）日：2009-08-27

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了一种可以调节Janus激酶活性的化合物，这些化合物可用于治疗与Janus激酶活性相关的疾病，例如免疫相关疾病和癌症。
• WO2006/137658
  申请人：——

  公开号：——

  公开（公告）日：——
• [EN] TETRACYCLIC INHIBITORS OF JANUS KINASES<br/>[FR] INHIBITEURS TETRACYCLIQUES DE JANUS KINASES
  申请人：INCYTE CORP

  公开号：WO2005105814A1

  公开（公告）日：2005-11-10

  The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

  本发明提供了能调节雅努斯激酶活性并且在治疗与雅努斯激酶活性相关的疾病方面有用的化合物，例如免疫相关疾病和癌症。
• Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis
  作者：Laszlo Revesz、Ernst Blum、Franco E. Di Padova、Thomas Buhl、Roland Feifel、Hermann Gram、Peter Hiestand、Ute Manning、Gerard Rucklin

  DOI：10.1016/j.bmcl.2004.03.106

  日期：2004.7

  A library of trisubstituted oxazoles, thiazoles, imidazoles (1,2,4- and 2,4,5-substituted) and imidazo[1,2-b]pyridines was prepared and evaluated in vitro as p38alpha inhibitors and in vivo in several models of rheumatoid arthritis. Four structures 32, 37, 45 and 59-were identified as potent inhibitors of p38alpha with high efficacy in the LPS induced TNFalpha release model in the mouse, the adjuvant induced arthritis and the collagen induced arthritis in the rat with ED(50)s between 1.0 and 9.5 mg/kg p.o. (C) 2004 Elsevier Ltd. All rights reserved.