triisopropyl-[(8-vinyl-2-naphthyl)oxy]silane | 497151-67-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: triisopropyl-[(8-vinyl-2-naphthyl)oxy]silane
• 英文别名: (8-ethenylnaphthalen-2-yl)oxy-tri(propan-2-yl)silane
• CAS: 497151-67-4
• 化学式: C₂₁H₃₀OSi
• 分子量: 326.554
• InChiKey: CCTWIHNJBNYIRU-UHFFFAOYSA-N

物化性质

• 沸点：
  392.2±11.0 °C(Predicted)
• 密度：
  0.953±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  7.04
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  9.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  triisopropyl-[(8-vinyl-2-naphthyl)oxy]silane 在 9-硼双环[3.3.1]壬烷 、 双氧水 、 sodium hydroxide 作用下， 以 四氢呋喃 、 水 为溶剂， 反应 11.0h， 以56%的产率得到2-{7-[(triisopropylsilyl)oxy]-1-naphthyl}ethanol
  参考文献：
  名称：

  Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence

  摘要：

  We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.04.013
• 作为产物：
  描述：

  1-氨基-7-萘酚 在 咪唑 、 potassium iodide 、 sodium nitrite 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 反应 33.0h， 生成 triisopropyl-[(8-vinyl-2-naphthyl)oxy]silane
  参考文献：
  名称：

  Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence

  摘要：

  We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.04.013

文献信息

• Amine derivatives
  申请人：——

  公开号：US20040259875A1

  公开（公告）日：2004-12-23

  An amine derivative, its tautomeric or stereoisomeric form, or a salt thereof which has vanilloid receptor 1 (VR1) antagonistic activity, is disclosed. The amine derivative has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

  本发明揭示了一种具有vanilloid receptor 1（VR1）拮抗活性的胺衍生物、其互变异构体或立体异构体形式或其盐。该胺衍生物具有优异的VR1拮抗活性，适用于预防和治疗与VR1活性相关的疾病，特别是用于治疗尿失禁、过度活动膀胱、慢性疼痛、神经痛、术后疼痛、类风湿性关节炎疼痛、神经痛、神经病、疼痛、神经损伤、缺血、神经退行性疾病、中风、失禁和/或炎症性疾病。
• Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence
  作者：Klaus Urbahns、Takeshi Yura、Muneto Mogi、Masaomi Tajimi、Hiroshi Fujishima、Tsutomu Masuda、Nagahiro Yoshida、Toshiya Moriwaki、Timothy B. Lowinger、Heinrich Meier、Fiona Chan、David Madge、Jang B. Gupta

  DOI：10.1016/j.bmcl.2011.04.013

  日期：2011.6

  We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced clearance, improved potency and is active in rat cystometry models of urinary incontinence after intravenous administration. (C) 2011 Elsevier Ltd. All rights reserved.