5-Trimethylsilylethynyl-3-(1-methyl-2-pyrrolidinyl) pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 5-Trimethylsilylethynyl-3-(1-methyl-2-pyrrolidinyl) pyridine
• 英文别名: 5-Trimethylsilylethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine；trimethyl-[2-[5-(1-methylpyrrolidin-2-yl)pyridin-3-yl]ethynyl]silane
• 化学式: C₁₅H₂₂N₂Si
• 分子量: 258.439
• InChiKey: UTBQXVHKOVFDCS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.08
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  16.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-Trimethylsilylethynyl-3-(1-methyl-2-pyrrolidinyl) pyridine 、 Dicaesio carbonate 在 乙酸乙酯 、 水 、 Brine 、 Sodium sulfate-III 、 crude product 、 silica gel 、 ethyl acetate n-hexane 作用下， 以 甲醇 为溶剂， 反应 5.0h， 以to afford 5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine as an oil, 218 mg, 59%的产率得到5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine
  参考文献：
  名称：

  Modulators of acetylcholine receptors

  摘要：

  本发明提供了一类吡啶化合物，它们是乙酰胆碱受体调节剂，即这些化合物可以从其结合位点上取代乙酰胆碱受体配体。发明化合物可以作为乙酰胆碱受体的激动剂、部分激动剂、拮抗剂或别构调节剂，并可用于各种治疗应用，如治疗阿尔茨海默病和其他涉及记忆丧失和/或痴呆的疾病；注意力和专注障碍；运动功能障碍；情绪和情感障碍；物质滥用，包括戒断综合征和替代疗法；神经内分泌障碍和食欲调节失常，包括贪食症和厌食症；疼痛感知和疼痛控制障碍；自主神经障碍，包括胃肠动力和功能障碍；嗜铬细胞瘤；心血管功能障碍，包括高血压和心律失常，手术程序中的联用药物等。

  公开号：

  US05723477A1

文献信息

• Methods for the preparation of modulators of acetylcholine receptors
  申请人：Sibia Neurosciences, Inc.

  公开号：US05677459A1

  公开（公告）日：1997-10-14

  In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

  根据本发明提供了一类吡啶化合物，这些化合物是乙酰胆碱受体的调节剂。本发明的化合物可以从其结合位点上排挤乙酰胆碱受体配体。发明的化合物可能作为乙酰胆碱受体的激动剂、部分激动剂、拮抗剂或变构调节剂，并且可用于各种治疗应用，如治疗阿尔茨海默病和其他涉及记忆丧失和/或痴呆的疾病（包括艾滋病痴呆）；注意力和专注障碍（如注意力缺陷障碍）；运动功能外围运动障碍，如帕金森病、亨廷顿病、吉尔·德·拉·图雷特综合症和迟发性运动障碍；情绪和情感障碍，如抑郁、恐慌、焦虑和精神病；物质滥用，包括戒断综合症和替代疗法；神经内分泌紊乱和食物摄入失调，包括暴食症和厌食症；疼痛感知和疼痛控制障碍；自主神经障碍，包括胃肠道运动和功能障碍，如炎症性肠病、肠易激综合症、腹泻、便秘、胃酸分泌和溃疡；嗜铬细胞瘤；心血管功能障碍，包括高血压和心律失常，手术过程中的联合用药等。
• Modulators of acetylcholine receptors
  申请人：SIBIA Neurosciences, Inc.

  公开号：US05594011A1

  公开（公告）日：1997-01-14

  g In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia; disorders of attention and focus; disorders of extrapyramidal motor function; mood and emotional disorders; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function; pheochromocytoma; cardiovascular dysfunction hypertension and cardia arrhythmias; comedication in surgical procedures, and the like.

  根据本发明，提供了一类吡啶化合物，它们是乙酰胆碱受体的调节剂。本发明的化合物可将乙酰胆碱受体配体从其结合位点上置换出来。本发明的化合物可作为乙酰胆碱受体的激动剂、部分激动剂、拮抗剂或变构调节剂，并可用于多种治疗应用，例如治疗阿尔茨海默病和其他涉及记忆丧失和/或痴呆的疾病；注意力和专注障碍；外展性运动功能障碍；情绪和情感障碍；物质滥用，包括戒断综合症和替代疗法；神经内分泌障碍和食物摄入失调；痛觉和疼痛控制障碍；自主神经障碍，包括胃肠动力和功能障碍；嗜铬细胞瘤；心血管功能障碍，高血压和心律失常；手术程序中的联合用药等。