trans-tert-butyl(1-oxaspiro[2.5]oct-6-yloxy)diphenylsilane

• 分子结构分类: 有机化合物 - 有机金属化合物 - 有机类金属化合物
• 英文名称: trans-tert-butyl(1-oxaspiro[2.5]oct-6-yloxy)diphenylsilane
• 英文别名: tert-Butyl(1-oxaspiro[2.5]oct-6-yloxy)diphenylsilane；tert-butyl-(1-oxaspiro[2.5]octan-6-yloxy)-diphenylsilane
• 化学式: C₂₃H₃₀O₂Si
• 分子量: 366.576
• InChiKey: XJMMSLWDHGDULG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.27
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  21.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  sodium;hydride 、 三甲基碘化亚砜 、 4-[[(1,1-二甲基乙基)二苯基甲硅烷基]氧基]-环己酮 在 乙醚 、 magnesium sulfate 、 silica gel 、 ethyl acetate n-hexane 作用下， 以 二甲基亚砜 、 水 为溶剂， 反应 2.5h， 以to give 459 mg (13%, trans) and 390 mg (11%, cis) of the title compound as a colorless oil respectively的产率得到trans-tert-butyl(1-oxaspiro[2.5]oct-6-yloxy)diphenylsilane
  参考文献：
  名称：

  Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity

  摘要：

  该发明提供了一种式(I)的化合物：其中，Het代表一个杂环基团，其中有一个氮原子，B直接结合到该氮原子上，该杂环基团具有4到7个碳原子，且该杂环基团未取代或被1到4个独立选择的取代基α1取代；A代表具有1到4个碳原子的烷基链；B代表共价键或具有1到5个碳原子的烷基链；R1代表异丙基基团、正丙基基团或环戊基基团；R2代表甲基基团、氟原子或氯原子；R3独立地表示（i）氧代基、羟基、氨基、烷基氨基或羧基；（ii）具有3到8个碳原子的环烷基团，该环烷基团被1到5个取代基取代；或（iii）具有3到8个原子的杂环基团，该杂环基团未取代或被1到5个取代基取代，n为1、2或3，或其药学上可接受的盐。这些化合物具有5-HT4受体激动活性，因此可用于哺乳动物，特别是人类的胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征等的治疗。

  公开号：

  US07964727B2

文献信息

• [EN] BENZIMIDAZOLONE COMPOUNDS HAVING 5-HT4 RECEPTOR AGONISTIC ACTIVITY<br/>[FR] COMPOSES DE BENZIMIDAZOLONE A ACTIVITE D'AGONISTES DU RECEPTEUR 5-HT4
  申请人：PFIZER JAPAN INC

  公开号：WO2005021539A1

  公开（公告）日：2005-03-10

  This invention provides a compound of the formula (I) or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

  该发明提供了式(I)的化合物或其药用可接受的盐，以及含有这种化合物的组合物和利用这种化合物制造用于治疗胃食管反流病、胃肠疾病、胃动力障碍、非溃疡性消化不良、功能性消化不良、肠易激综合征（IBS）、便秘、消化不良、食管炎、胃食管疾病、恶心、中枢神经系统疾病、阿尔茨海默病、认知障碍、呕吐、偏头痛、神经系统疾病、疼痛、心血管疾病、心力衰竭、心律失常、糖尿病和呼吸暂停综合征的药物的用途。这些化合物具有5-HT4受体激动活性，因此对于治疗哺乳动物，尤其是人类的胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征等疾病是有用的。
• Quinolonecarboxylic Acid Compounds Having 5-Ht4 Receptor Agonistic Activity
  申请人：Kato Tomoki

  公开号：US20080255113A1

  公开（公告）日：2008-10-16

  This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α 1 ; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R 1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R 2 represents a methyl group, a fluorine atom or a chlorine atom; R 3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT 4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

  本发明提供了式（I）的化合物：其中，Het代表具有一个氮原子的杂环基团，与B直接结合，具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基独立地选自α1取代基组成的基团取代；A代表具有1至4个碳原子的脂肪族基团；B代表共价键或具有1至5个碳原子的脂肪族基团；R1代表异丙基基团、正丙基基团或环戊基团；R2代表甲基基团、氟原子或氯原子；R3独立地代表（i）氧代基、羟基、氨基、烷基氨基或羧基；（ii）具有3至8个碳原子的环烷基团，所述环烷基团被1至5个取代基取代；或（iii）具有3至8个原子的杂环基团，所述杂环基团未被取代或被1至5个取代基独立地选自α1取代基组成的基团取代，n为1、2或3，或其药学上可接受的盐。这些化合物具有5-HT4受体激动活性，因此对于哺乳动物，特别是人类的治疗胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征等非常有用。
• Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity
  申请人：Pfizer Inc.

  公开号：US07964727B2

  公开（公告）日：2011-06-21

  This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.

  该发明提供了一种式(I)的化合物：其中，Het代表一个杂环基团，其中有一个氮原子，B直接结合到该氮原子上，该杂环基团具有4到7个碳原子，且该杂环基团未取代或被1到4个独立选择的取代基α1取代；A代表具有1到4个碳原子的烷基链；B代表共价键或具有1到5个碳原子的烷基链；R1代表异丙基基团、正丙基基团或环戊基基团；R2代表甲基基团、氟原子或氯原子；R3独立地表示（i）氧代基、羟基、氨基、烷基氨基或羧基；（ii）具有3到8个碳原子的环烷基团，该环烷基团被1到5个取代基取代；或（iii）具有3到8个原子的杂环基团，该杂环基团未取代或被1到5个取代基取代，n为1、2或3，或其药学上可接受的盐。这些化合物具有5-HT4受体激动活性，因此可用于哺乳动物，特别是人类的胃食管反流病、非溃疡性消化不良、功能性消化不良、肠易激综合征等的治疗。