1-(t-Butyldimethylsiloxy)-4-(3-amino-phenyl)-3-butyne

• 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: 1-(t-Butyldimethylsiloxy)-4-(3-amino-phenyl)-3-butyne
• 英文别名: 3-[4-[tert-butyl(dimethyl)silyl]oxybut-1-ynyl]aniline
• 化学式: C₁₆H₂₅NOSi
• 分子量: 275.466
• InChiKey: JMUOGYXVSRJRSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.03
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  4-(叔丁基二甲基硅杂氧基)-1-丁炔 、 间溴苯胺 在 四(三苯基膦)钯 氮气 、 二氯甲烷 、 碳酸氢钠 、 magnesium sulfate 作用下， 以 正丁胺 为溶剂， 反应 18.0h， 生成 1-(t-Butyldimethylsiloxy)-4-(3-amino-phenyl)-3-butyne
  参考文献：
  名称：

  4-substituted piperidine analogs and their use as subtype selective NMDA

  摘要：

  本文介绍了新型4-取代哌啶类似物、含有它们的药物组合物以及使用4-取代哌啶类似物作为选择性活性N-甲基-D-天门冬氨酸（NMDA）受体亚型拮抗剂治疗中风、脑缺血、中枢神经系统创伤、低血糖、焦虑、惊厥、氨基糖苷类抗生素引起的听力损失、偏头痛、青光眼、巨细胞病毒视网膜炎、慢性疼痛、阿片类药物耐受或戒断以及神经退行性疾病，如狼麻痹、阿尔茨海默病、帕金森病和亨廷顿病的条件。同时，还介绍了制备4-取代哌啶类似物的新方法和4-取代哌啶类似物的新中间体。

  公开号：

  US06130234A1

文献信息

• 4-substituted piperidine analogs and their use as subtype selective NMDA
  申请人：Warner-Lambert Company

  公开号：US06130234A1

  公开（公告）日：2000-10-10

  Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

  新型4-取代哌啶类似物，含有这些类似物的药物组合物以及将4-取代哌啶类似物作为选择性活性N-甲基-D-天冬氨酸（NMDA）受体亚型拮抗剂治疗中风、脑缺血、中枢神经系统创伤、低血糖、焦虑、抽搐、氨基糖苷类抗生素引起的听力损失、偏头痛、青光眼、巨细胞病毒性视网膜炎、慢性疼痛、阿片类耐受性或戒断症状，或神经退行性疾病，如拉蒂病、阿尔茨海默病、帕金森病和亨廷顿病的治疗方法被描述。还描述了制备4-取代哌啶类似物的新方法以及4-取代哌啶类似物的新中间体。
• 4-substituted piperidine analogs and their use as subtype selective NMDA receptor antagonists
  申请人：Warner-Lambert Company

  公开号：US06448270B1

  公开（公告）日：2002-09-10

  Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using the 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as cerebral ischemia, central nervous system trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headaches, convulsions, aminoglycoside antibiotics-induced hearing loss, chronic pain, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, urinary incontinence and neurodegenerative disorders such as lathyrism, Alzheimers' Disease, Parkinsonism, and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

  本发明涉及一种新型的4-取代哌啶类似物、含有它们的制药组合物以及使用这些4-取代哌啶类似物作为选择性活性N-甲基-D-天门冬氨酸（NMDA）受体亚型拮抗剂来治疗脑缺血、中枢神经系统创伤、低血糖、神经退行性疾病、焦虑、偏头痛、惊厥、氨基糖苷类抗生素引起的听力损失、慢性疼痛、精神病、青光眼、巨细胞病毒性视网膜炎、阿片类耐受或戒断、尿失禁以及神经退行性疾病，例如荚藤病、阿尔茨海默病、帕金森病和亨廷顿病的方法。本发明还涉及制备4-取代哌啶类似物的新方法以及4-取代哌啶类似物的新中间体。
• 4-Substituted piperidine analogs and their use as subtype selective NMDA receptor, antagonists
  申请人：——

  公开号：US20030105133A1

  公开（公告）日：2003-06-05

  Novel 4-substituted piperidine analogs, pharmaceutical compositions containing the same and the method of using 4-substituted piperidine analogs as selectively active antagonists of N-methyl-D-aspartate (NMDA) receptor subtypes for treating conditions such as stroke, cerebral ischemia, central nervous system trauma, hypoglycemia, anxiety, convulsions, aminoglycoside antibiotics-induced hearing loss, migraine headaches, glaucoma, CMV retinitis, chronic pain, opioid tolerance or withdrawals, or neurodegenerative disorders, such as lathyrism, Alzheimer's Disease, Parkinsonism and Huntington's Disease are described. Also described are novel methods for preparing 4-substituted piperidine analogs and novel intermediates of the 4-substituted piperidine analogs.

  本文介绍了新型4-取代哌啶类似物、含有相同成分的制药组合物以及使用4-取代哌啶类似物作为选择性活性N-甲基-D-天门冬氨酸（NMDA）受体亚型拮抗剂治疗中风、脑缺血、中枢神经系统创伤、低血糖、焦虑、惊厥、氨基糖苷类抗生素引起的听力损失、偏头痛、青光眼、巨细胞病毒性视网膜炎、慢性疼痛、阿片类耐受或戒断综合征或神经退行性疾病，如拉蒂病、阿尔茨海默病、帕金森病和亨廷顿病的条件。还介绍了制备4-取代哌啶类似物的新方法和4-取代哌啶类似物的新中间体。