3-amino-1-adamantanecarbonyl chloride | 428816-49-3

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 酰卤
• 英文名称: 3-amino-1-adamantanecarbonyl chloride
• 英文别名: 1-Aza-5-methyladamantane-3-carbonyl chloride；3-aminoadamantane-1-carbonyl chloride
• CAS: 428816-49-3
• 化学式: C₁₁H₁₆ClNO
• 分子量: 213.707
• InChiKey: KEPRABDVMDKGFP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  43.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-amino-1-adamantanecarbonyl chloride 在 sodium hydroxide 、 硫酸 、 水 、 溶剂黄146 作用下， 以 甲苯 为溶剂， 反应 1.0h， 生成 1-acetyl-3-aminoadamantane
  参考文献：
  名称：

  摘要：

  A general procedure was proposed for synthesizing 3-R-1-adamantyl methyl ketones from the corresponding adamantanecarbonyl chlorides and dimethyl malonate in toluene (benzene) in the presence of sodium hydroxide. Intermediate dimethyl (3-R-1-adamantylcarbonyl)malonates can also be isolated. The resulting ketones were brought into reactions with hydroxylamine and formamide in the presence of formic acid to obtain the corresponding oximes and 1-(3-R-1-adamantyl)ethylamines. Dimethyl (3-R-1-adamantylcarbonyl)malonates reacted with phenylhydrazine to give adamantyl-substituted 4,5-dihydropyrazol-5-one derivatives.

  DOI：

  10.1023/a:1013154831862

文献信息

• Pyrrolidine compounds and medicinal utilization thereof
  申请人：Mitsubishi Pharma Corporation

  公开号：US06468998B1

  公开（公告）日：2002-10-22

  The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.

  本发明提供了一种式（I）的吡咯烷化合物，其中每个符号如规范中所定义，以及其光学活性化合物和药学上可接受的盐。本发明还提供了一种含有式（I）化合物、其光学活性化合物或药学上可接受的盐以及药学上可接受的添加剂的制药组合物。本发明所述化合物具有血清素2受体拮抗作用以及抑制血小板聚集、改善外周循环和促进泪液分泌的作用。因此，本发明所述化合物可以是一种有益的药物，具有对抗血栓栓塞、干眼症等疾病的作用。
• PYRROLIDINE COMPOUNDS AND MEDICINAL UTILIZATION THEREOF
  申请人：Welfide Corporation

  公开号：EP1125922A1

  公开（公告）日：2001-08-22

  The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.

  本发明提供了一种式 (I) 的吡咯烷化合物 其中各符号如说明书中所定义，其光学活性化合物及其药学上可接受的盐。本发明进一步提供了含有式（I）化合物、其光学活性化合物或其药学上可接受的盐以及药学上可接受的添加剂的药物组合物。本发明的化合物具有 5-羟色胺 2 受体拮抗作用、血小板聚集抑制作用、外周循环改善作用和流泪促进作用。因此，本发明的化合物可以作为一种有用的药物，对血栓性栓塞、干眼症等具有疗效。
• US6468998B1
  申请人：——

  公开号：US6468998B1

  公开（公告）日：2002-10-22
• ——
  作者：V. V. Pozdnyakov、N. V. Makarova、I. K. Moiseev

  DOI：10.1023/a:1013154831862

  日期：——

  A general procedure was proposed for synthesizing 3-R-1-adamantyl methyl ketones from the corresponding adamantanecarbonyl chlorides and dimethyl malonate in toluene (benzene) in the presence of sodium hydroxide. Intermediate dimethyl (3-R-1-adamantylcarbonyl)malonates can also be isolated. The resulting ketones were brought into reactions with hydroxylamine and formamide in the presence of formic acid to obtain the corresponding oximes and 1-(3-R-1-adamantyl)ethylamines. Dimethyl (3-R-1-adamantylcarbonyl)malonates reacted with phenylhydrazine to give adamantyl-substituted 4,5-dihydropyrazol-5-one derivatives.