2-bromo-N-(2,4,6-tribromo-3-methylphenyl)acetamide | 630120-36-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-bromo-N-(2,4,6-tribromo-3-methylphenyl)acetamide
• CAS: 630120-36-4
• 化学式: C₉H₇Br₄NO
• 分子量: 464.777
• InChiKey: VXBQYVDGDUPARJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2-bromo-N-(2,4,6-tribromo-3-methylphenyl)acetamide 在 palladium on activated charcoal 超重氢 、 三乙胺 、 N,N-二异丙基乙胺 作用下， 以 乙酸乙酯 、 甲苯 为溶剂， 反应 2.5h， 生成 [3H]-A 369508
  参考文献：
  名称：

  Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand

  摘要：

  The first selective dopamine D-4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands was measured and [H-3]6b found to be suitable for use in D-4 saturation and competition binding studies. The synthesis, biological, and radioactivity of this new agonist radioligand as well as preliminary SAR will be discussed. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.07.068
• 作为产物：
  描述：

  溴乙酰氯 、 3-甲基-2,4,6-三溴苯胺 以 甲苯 为溶剂， 反应 24.0h， 以to provide 2.88 g (49%) of the title compound as a white solid的产率得到2-bromo-N-(2,4,6-tribromo-3-methylphenyl)acetamide
  参考文献：
  名称：

  Acetamides and benzamides that are useful in treating sexual dysfunction

  摘要：

  本发明涉及使用式(I)的化合物治疗性功能障碍以及含有式(I)的化合物的组合物治疗性功能障碍。

  公开号：

  US20060009461A1

文献信息

• Acetamides and benzamides that are useful in treating sexual dysfunction
  申请人：——

  公开号：US20040029887A1

  公开（公告）日：2004-02-12

  The present invention relates to the use of compounds of formula (I) 1 for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.

  本发明涉及使用式(I)的化合物治疗性功能障碍，以及含有式(I)化合物的组合物用于治疗性功能障碍。
• ACETAMIDES AND BENZAMIDES THAT ARE USEFUL IN TREATING SEXUAL DYSFUNCTION
  申请人：Abbott Laboratories

  公开号：EP1509213A2

  公开（公告）日：2005-03-02
• US7528134B2
  申请人：——

  公开号：US7528134B2

  公开（公告）日：2009-05-05
• [EN] ACETAMIDES AND BENZAMIDES THAT ARE USEFUL IN TREATING SEXUAL DYSFUNCTION<br/>[FR] ACETAMIDES ET BENZAMIDES UTILISES DANS LE TRAITEMENT D'UNE DYSFONCTION SEXUELLE
  申请人：ABBOTT LAB

  公开号：WO2003099266A2

  公开（公告）日：2003-12-04

  The present invention relates to the use of compounds of formula (I), for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.
• Synthesis and activity of 2-[4-(4-[3H]-2-cyanophenyl)piperazinyl]-N-(2,4,6-[3H]3-3-methylphenyl)acetamide: a selective dopamine D4 receptor agonist and radioligand
  作者：Mark A. Matulenko、Bruce Surber、Leimin Fan、Teodozyi Kolasa、Masaki Nakane、Marc A. Terranova、Marie E. Uchic、Loan N. Miller、Renjie Chang、Diana L. Donnelly-Roberts、Marian T. Namovic、Robert B. Moreland、Jorge D. Brioni、Andrew O. Stewart

  DOI：10.1016/j.bmcl.2004.07.068

  日期：2004.10

  The first selective dopamine D-4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands was measured and [H-3]6b found to be suitable for use in D-4 saturation and competition binding studies. The synthesis, biological, and radioactivity of this new agonist radioligand as well as preliminary SAR will be discussed. (C) 2004 Elsevier Ltd. All rights reserved.