1-(2,3,5,6-tetrafluoropyridin-4-yl)piperazine | 777845-60-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(2,3,5,6-tetrafluoropyridin-4-yl)piperazine
• CAS: 777845-60-0
• 化学式: C₉H₉F₄N₃
• 分子量: 235.184
• InChiKey: QCKDBJQSKIOGOY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  28.2
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  1-(2,3,5,6-tetrafluoropyridin-4-yl)piperazine 、 p-(dimethylamino)salicylic acid methyl ester 在 caesium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成
  参考文献：
  名称：

  Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)

  摘要：

  In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, was replaced with a primary amine. Further modifications led to the identification of potent, selective, and orally bioavailable uPA inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.08.008
• 作为产物：
  描述：

  1-(2,3,5,6-tetrafluoropyridin-4-yl)-4-benzylpiperazine 在 氯甲酸氯乙酯 作用下， 以 1,2-二氯乙烷 、 甲醇 为溶剂， 反应 4.58h， 生成 1-(2,3,5,6-tetrafluoropyridin-4-yl)piperazine
  参考文献：
  名称：

  Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by np y5 receptor

  摘要：

  式(I)的化合物： 其中： X是式(A)或(B)的基团： 而R1、R2、R3、R4、n、x、y和z的定义如所述。 还描述了它们的制备过程以及它们在治疗由神经肽Y5受体介导的疾病中的用途，如在温血动物，如人类中的用途。

  公开号：

  US20030225097A1

文献信息

• Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by np y5 receptor
  申请人：——

  公开号：US20030225097A1

  公开（公告）日：2003-12-04

  Compounds of formula (I): 1 wherein: X is a group of formula (A) or (B): 2 and R 1 , R 2 , R 3 , R 4 , n, x, y and z are as defined within are described. Processes for their preparation and their use in the treatment of disorders mediated by the neuropeptide Y5 receptor in a warm-blooded animal, such as a human being are also described.

  式(I)的化合物： 其中： X是式(A)或(B)的基团： 而R1、R2、R3、R4、n、x、y和z的定义如所述。 还描述了它们的制备过程以及它们在治疗由神经肽Y5受体介导的疾病中的用途，如在温血动物，如人类中的用途。
• Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)
  作者：Christopher W. West、Marc Adler、Danny Arnaiz、Deborah Chen、Kieu Chu、Giovanna Gualtieri、Elena Ho、Christoph Huwe、David Light、Gary Phillips、Rebecca Pulk、Drew Sukovich、Marc Whitlow、Shendong Yuan、Judi Bryant

  DOI：10.1016/j.bmcl.2009.08.008

  日期：2009.10

  In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provided compounds in which the amidine, binding in the S1 pocket, was replaced with a primary amine. Further modifications led to the identification of potent, selective, and orally bioavailable uPA inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.