Cyclopropylmethyl-(2,2,3,3,3-pentafluoro-propyl)-amine | 749201-08-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: Cyclopropylmethyl-(2,2,3,3,3-pentafluoro-propyl)-amine
• 英文别名: N-(2,2,3,3,3-Pentafluoropropyl)cyclopropanemethanamine；N-(cyclopropylmethyl)-2,2,3,3,3-pentafluoropropan-1-amine
• CAS: 749201-08-9
• 化学式: C₇H₁₀F₅N
• 分子量: 203.155
• InChiKey: OKJZXXQGXCWMSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  12
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  Cyclopropylmethyl-(2,2,3,3,3-pentafluoro-propyl)-amine 在 三甲基铝 、 红铝 作用下， 以 甲苯 为溶剂， 反应 38.0h， 生成 Cyclopropylmethyl-(2,2,3,3,3-pentafluoro-propyl)-[2-trifluoromethyl-9-(2,4,6-trimethyl-phenyl)-9H-benzo[d]imidazo[1,2-a]imidazol-3-ylmethyl]-amine
  参考文献：
  名称：

  Synthesis and structure–activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists

  摘要：

  8-Aryl-1,3a,8-triaza-cyclopenta[a]indenes represent a novel series of high binding affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis, SAR, and pharmacokinetic properties of compound 8e (K-i = 23 nM). (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.06.028

文献信息

• Synthesis, structure–activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists
  作者：Xiaojun Han、Jodi A. Michne、Sokhom S. Pin、Kevin D. Burris、Lynn A. Balanda、Lawrence K. Fung、Tracey Fiedler、Kaitlin E. Browman、Matthew T. Taber、Jie Zhang、Gene M. Dubowchik

  DOI：10.1016/j.bmcl.2005.05.117

  日期：2005.9

  7-Aryl-6,7-dihydroimidazoimidazoles represent a novel series of high-affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis and SAR as well as behavioral activity of two exemplary compounds, 7b and 7k, in a mouse canopy model of anxiety.

  7-芳基-6,7-二氢咪唑并咪唑代表了一系列新的高亲和性促肾上腺皮质激素释放因子1受体拮抗剂。在这里，我们报告了它们的合成和SAR以及两个示例性化合物7b和7k在焦虑的小鼠冠层模型中的行为活性。
• [EN] SUBSTITUTED AZOLE DERIVATIVES AS INHIBITORS OF CORTICOTROPIN RELEASING FACTOR<br/>[FR] DERIVES D'AZOLE SUBSTITUES EN TANT QU'INHIBITEURS DU FACTEUR DE LIBERATION DE LA CORTICOTROPINE
  申请人：BRISTOL MYERS SQUIBB CO

  公开号：WO2002024200A1

  公开（公告）日：2002-03-28

  The present invention relates to thiazoles, oxazoles, imidazoles and pharmaceutical compositions comprising said compounds antagonizing the corticotropin releasing factor receptor ('CRF receptor') and useful for the treatment of depression, anxiety, affective disorders, feeding disorders, post-traumatic stress disorder, headache, drug addiction, inflammatory disorders, drug or alcohol withdrawal symptoms and other conditions the treatment of which can be affected by the antagonism of the CRF-1 receptor.

  本发明涉及噻唑、噁唑、咪唑及包含该类化合物的药物组合物，其对促肾上腺皮质激素释放因子受体（“CRF受体”）具有拮抗作用，并且可用于治疗抑郁症、焦虑症、情感障碍、进食障碍、创伤后应激障碍、头痛、药物成瘾、炎症性疾病、药物或酒精戒断症状以及其他可能受CRF-1受体拮抗作用影响的疾病的治疗。
• EP1320365A4
  申请人：——

  公开号：EP1320365A4

  公开（公告）日：2004-03-17
• SUBSTITUTED AZOLE DERIVATIVES AS INHIBITORS OF CORTICOTROPIN RELEASING FACTOR
  申请人：Bristol-Myers Squibb Co.

  公开号：EP1320365A1

  公开（公告）日：2003-06-25
• Synthesis and structure–activity relationship of imidazo[1,2-a]benzimidazoles as corticotropin-releasing factor 1 receptor antagonists
  作者：Xiaojun Han、Sokhom S. Pin、Kevin Burris、Lawrence K. Fung、Stella Huang、Matthew T. Taber、Jie Zhang、Gene M. Dubowchik

  DOI：10.1016/j.bmcl.2005.06.028

  日期：2005.9

  8-Aryl-1,3a,8-triaza-cyclopenta[a]indenes represent a novel series of high binding affinity corticotropin-releasing factor 1 receptor antagonists. Here, we report their synthesis, SAR, and pharmacokinetic properties of compound 8e (K-i = 23 nM). (c) 2005 Elsevier Ltd. All rights reserved.