(+)-2-benzyloxy-2-phenylethylamine

• 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: (+)-2-benzyloxy-2-phenylethylamine
• 英文别名: 2-Benzyloxy-2-phenylethylamine；2-phenyl-2-phenylmethoxyethanamine
• 化学式: C₁₅H₁₇NO
• 分子量: 227.306
• InChiKey: QSFQGTSBZYUMMO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  isopropyl N-cyano-3-pyridinecarboximidate 、 (+)-2-benzyloxy-2-phenylethylamine 在 chloroform methanol 作用下， 以 甲醇 为溶剂， 反应 3.0h， 以to give N-cyano-N'-(2-benzyloxy-2-phenylethyl)-3-pyridinecarboximidamide (0.24 g, 0.7 mmol, yield: 64%) as colorless syrup的产率得到N-cyano-N'-(2-benzyloxy-2-phenylethyl)-3-pyridinecarboximidamide
  参考文献：
  名称：

  Pyridyl carboximidamide compounds useful in treating blood pressure

  摘要：

  本发明公开了以下式（A）所代表的新型羧酸亚胺衍生物及其酸加合物盐：##STR1## 其中所有取代基的含义与上述定义相同。本发明还公开了以下式（II）所代表的N-氰基吡啶羧酸亚胺化合物，它们是制备N-氰基-N'-取代吡啶羧酸亚胺衍生物中取代基B为吡啶的中间体：##STR2## 其中所有取代基的含义与上述定义相同。本发明还公开了制备这些化合物的方法，包括具有扩血管作用的化合物的制药剂以及在治疗中对患者进行化合物剂量的治疗方法。

  公开号：

  US05223508A1
• 作为产物：
  描述：

  苯甲醇钠 在 platinum on activated charcoal 氢气 作用下， 以 乙醇 、 苯甲醇 为溶剂， 25.0 ℃ 、101.33 kPa 条件下， 反应 20.0h， 生成 (+)-2-benzyloxy-2-phenylethylamine
  参考文献：
  名称：

  β-Alkoxy-substituted phenethylamines: a family of compounds potentially active at the dopamine and α-adrenergic receptors

  摘要：

  A series of beta-alkoxy-substituted phenethylamines were synthesized and tested for their affinity at the D-1 and D-2 dopaminergic receptors and the alpha(1) and alpha(2) adrenoceptors. None of the tested compounds exhibited D-2 receptor affinity. Among the nonhydroxylated compounds that were resolved to their antipodes, the (-)-enantiomers generally showed a moderate but distinct activity at the alpha(2) receptor. Ring hydroxylation appears to be a necessary requirement for D-1, activity. These results are discussed in terms of the structural elements of the tested drugs as compared to those of known active compounds.

  DOI：

  10.1016/0223-5234(96)88314-0

文献信息

• Pyridyl carboximidamide compounds useful in treating blood pressure
  申请人：Kirin Beer Kabushiki Kaisha

  公开号：US05223508A1

  公开（公告）日：1993-06-29

  Novel carboximidamide derivatives represented by the following formula (A) and acid adduct salts thereof are disclosed: ##STR1## wherein all the substituents have the same meanings as defined above. N-cyano-pyridinecarboxyimidate compounds represented by the following formula (II) which are the intermediates for preparing of N-cyano-N'-substituted-pyridinecarboximidamide derivatives wherein the substituent B in the above described formula (A) is pyridine are also disclosed: ##STR2## wherein all the substituents have the same meanings as defined above. The process for preparing the compounds, the pharmaceutical agents comprising the compound having vasodilating effect, and the therapeutic method of dosing the compound on patients for therapy are also disclosed.

  本发明公开了以下式（A）所代表的新型羧酸亚胺衍生物及其酸加合物盐：##STR1## 其中所有取代基的含义与上述定义相同。本发明还公开了以下式（II）所代表的N-氰基吡啶羧酸亚胺化合物，它们是制备N-氰基-N'-取代吡啶羧酸亚胺衍生物中取代基B为吡啶的中间体：##STR2## 其中所有取代基的含义与上述定义相同。本发明还公开了制备这些化合物的方法，包括具有扩血管作用的化合物的制药剂以及在治疗中对患者进行化合物剂量的治疗方法。
• US5166347A
  申请人：——

  公开号：US5166347A

  公开（公告）日：1992-11-24
• US5223508A
  申请人：——

  公开号：US5223508A

  公开（公告）日：1993-06-29
• US5272164A
  申请人：——

  公开号：US5272164A

  公开（公告）日：1993-12-21
• β-Alkoxy-substituted phenethylamines: a family of compounds potentially active at the dopamine and α-adrenergic receptors
  作者：H.E. Katerinopoulos、N Tagmatarchis、G Zaponakis、N Kefalakis、K Kordatos、M Spyrakis、K Thermos

  DOI：10.1016/0223-5234(96)88314-0

  日期：1995.1

  A series of beta-alkoxy-substituted phenethylamines were synthesized and tested for their affinity at the D-1 and D-2 dopaminergic receptors and the alpha(1) and alpha(2) adrenoceptors. None of the tested compounds exhibited D-2 receptor affinity. Among the nonhydroxylated compounds that were resolved to their antipodes, the (-)-enantiomers generally showed a moderate but distinct activity at the alpha(2) receptor. Ring hydroxylation appears to be a necessary requirement for D-1, activity. These results are discussed in terms of the structural elements of the tested drugs as compared to those of known active compounds.