1-(丁-3-炔基)-2-甲基吡咯烷 | 1055997-20-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 1-(丁-3-炔基)-2-甲基吡咯烷
• 英文名称: 1-(but-3-ynyl)-2-methylpyrrolidine
• 英文别名: 1-But-3-ynyl-2-methyl-pyrrolidine；1-but-3-ynyl-2-methylpyrrolidine
• CAS: 1055997-20-0
• 化学式: C₉H₁₅N
• 分子量: 137.225
• InChiKey: NTVFDRLNCQVBCW-UHFFFAOYSA-N

物化性质

• 沸点：
  185.4±23.0 °C(Predicted)
• 密度：
  0.890±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  1-(丁-3-炔基)-2-甲基吡咯烷 、 4 -溴- 2 - 碘苯甲胺 以to provide 4-bromo-2-[4-(2-methyl-pyrrolidin-1-yl )-but-1-ynyl]-phenylamine (45)的产率得到4-bromo-2-[4-(2-methyl-pyrrolidin-1-yl)-but-1-ynyl]-phenylamine
  参考文献：
  名称：

  FUSED BICYCLIC-SUBSTITUTED AMINES AS HISTAMINE-3 RECEPTOR LIGANDS

  摘要：

  式(I)的化合物在治疗由组胺-3受体配体预防或改善的疾病或疾病中有用。此外，还披露了包含组胺-3受体配体的药物组合物以及使用这些化合物和组合物的方法。

  公开号：

  US20080119520A1
• 作为产物：
  描述：

  对甲苯磺酸 3-丁炔酯 、 2-甲基吡咯烷 生成 1-(丁-3-炔基)-2-甲基吡咯烷
  参考文献：
  名称：

  An efficient and convergent synthesis of the potent and selective H3 antagonist ABT-239

  摘要：

  An efficient and convergent process for the preparation of a potent and selective H-3 receptor antagonist, ABT-239, 1A was accomplished with an overall yield of 64%. The key step in the synthesis is a Sonogashira coupling/cyclization reaction of 1-but-3-ynyl-2-(R)-methylpyrrolidine (9) with 4'-hydroxy-3'-iodo-biphenyl-4-carbonitrile (3). Additionally, the key amine component 2-(R)-methylpyrrolidine (7) was effectively synthesized from the readily available Boc-L-prolinol with a simple catalytical hydrogenolysis as the key step. This column chromatography-free process is highlighted by several simple work-up and purification procedures and is amendable to the large-scale preparation of 1A. (c) 2006 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2006.02.046

文献信息

• Fused bicyclic-substituted amines as histamine-3 receptor ligands
  申请人：——

  公开号：US20040248899A1

  公开（公告）日：2004-12-09

  Compounds of formula (I) 1 are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.

  公式(I)1的化合物在治疗由组胺-3受体配体预防或改善的状况或疾病中是有用的。还公开了包含组胺-3受体配体的药物组合物以及使用这些化合物和组合物的方法。
• Novel amines as histamine-3 receptor ligands and their therapeutic applications
  申请人：——

  公开号：US20020169188A1

  公开（公告）日：2002-11-14

  Compounds of formula (I) 1 or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.

  化合物的公式(I)1或其药用可接受的盐或前药，对哺乳动物的组胺-3受体进行调节是有用的，并且对组胺-3受体配体改善的疾病的治疗是有用的。
• Fused Bicyclic-Substituted Amines as Histamine-3 Receptor Ligands
  申请人：COWART Marlon D.

  公开号：US20120108637A1

  公开（公告）日：2012-05-03

  Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.

  公式（I）的化合物可用于治疗由组胺-3受体配体防止或改善的病症或障碍。还公开了包含组胺-3受体配体的药物组合物以及使用这种化合物和组合物的方法。
• Amines as histamine-3 receptor ligands and their therapeutic applications
  申请人：Abbott Laboratories

  公开号：EP2258694A1

  公开（公告）日：2010-12-08

  Compounds of formula (I), or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders ameliorated by histamine-3 receptor ligands.

  式(I)化合物或其药学上可接受的盐、酯、酰胺或原药，可用于调节哺乳动物体内的组胺-3 受体，并可用于治疗组胺-3 受体配体可改善的疾病。
• NOVEL AMINES AS HISTAMINE-3 RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS
  申请人：Abbott Laboratories

  公开号：EP1370546A2

  公开（公告）日：2003-12-17