2-(2,3-环氧-丙氧基)-苯甲酸酰胺 | 34249-94-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 2-(2,3-环氧-丙氧基)-苯甲酸酰胺
• 英文名称: 2-(2,3-epoxy-propoxy)-benzoic acid amide
• 英文别名: 2-(2,3-Epoxy-propoxy)-benzoesaeure-amid；1-(2-carbamoylphenoxy)-2,3-epoxypropane；1-(o-Carbamoylphenoxy)-2,3-epoxypropane；2-(oxiran-2-ylmethoxy)benzamide
• CAS: 34249-94-0
• 化学式: C₁₀H₁₁NO₃
• 分子量: 193.202
• InChiKey: MIMIAWUVJMSJEJ-UHFFFAOYSA-N

物化性质

• 熔点：
  215.8-217.8 °C(Solv: water (7732-18-5))
• 沸点：
  372.5±17.0 °C(Predicted)
• 密度：
  1.267±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  64.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(2,3-环氧-丙氧基)-苯甲酸酰胺 生成 2-{2-Hydroxy-3-[2-(2-phenylacetylamino-acetylamino)-ethylamino]-propoxy}-benzamide
  参考文献：
  名称：

  DE2745222

  摘要：

  公开号：
• 作为产物：
  描述：

  水杨酰胺 在 哌啶 、 sodium hydroxide 作用下， 以 四氢呋喃 为溶剂， 反应 0.67h， 生成 2-(2,3-环氧-丙氧基)-苯甲酸酰胺
  参考文献：
  名称：

  Antihypertensive indole derivatives of phenoxypropanolamines with .beta.-adrenergic receptor antagonist and vasodilating activity

  摘要：

  A series of 25 aryloxypropanolamines containing the 3-indolyl-tert-butyl [i.e., 1,1-dimethyl-2-(1H-indol-3-yl)ethyl] or substituted 3-indolyl-tert-butyl moiety as the N substituent is reported. These compounds have been tested for antihypertensive activity in spontaneously hypertensive rats (SHR), beta-adrenergic receptor antagonist action in conscious normotensive rats, vasodilating activity in ganglion-blocked rats with blood pressure maintained by angiotensin II infusion, and for intrinsic sympathomimetic action (ISA) in reserpinized rats. Some of the compounds exhibit antihypertensive activity in combination with beta adrenergic receptor antagonist and vasodilating action. The structure--activity relationships in these tests are discussed.

  DOI：

  10.1021/jm00177a015

文献信息

• .beta.-Adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols
  作者：M. S. Large、L. H. Smith

  DOI：10.1021/jm00354a005

  日期：1982.12

  The synthesis of a series of 1-(aryloxy)-3-[[(amido)alkyl]amino] propan-2-ols where either the aryl moiety is heterocyclic or the amidic group is substituted by a heterocyclic moiety is described. Several of the compounds were more potent than propranolol when given intravenously to anesthetized rats. In contrast to previous findings with beta-blockers based on heterocyclic moieties and with either

  描述了一系列1-（芳氧基）-3-[[（（酰胺基烷基）氨基]氨基]丙-2-醇的合成，其中芳基部分为杂环或酰胺基被杂环部分取代。静脉给予麻醉大鼠时，几种化合物比普萘洛尔更有效。与先前基于杂环基团的β受体阻滞剂以及侧链具有异丙基氨基或叔丁基氨基取代基的先前发现相反，当在麻醉的猫中进一步检查时，几种化合物被证明具有心脏选择性。讨论了该系列化合物显示的详细的构效关系。
• Phenoxypropanolpiperazines
  申请人：Pfizer Inc.

  公开号：US03951983A1

  公开（公告）日：1976-04-20

  A series of novel substituted phenoxypropyl piperazine derivatives have been prepared by reacting the appropriate 1-phenoxy-2,3-epoxypropane compound with 1-phenoxy-3-(4-phenylpiperazine-1-yl)propan-2-ols suitable N-phenylpiperazine reagent. The resulting 1-phenoxy13-(4-phenylpiperazine-1-yl)propan-2-ols are useful in the field of chemotherapy as antihypertensive agents. Preferred members include compounds having an acetamidomethyl, carboxymethyl or carbamoylmethyl group substituted on the phenyl ring of the phenoxy moiety. Alternate methods of preparation are also provided.

  一系列新型取代的苯氧基丙基哌嗪衍生物已通过将适当的1-苯氧基-2,3-环氧丙烷化合物与1-苯氧基-3-(4-苯基哌嗪-1-基)丙烷-2-醇合适的N-苯基哌嗪试剂反应而制备。所得的1-苯氧基-3-(4-苯基哌嗪-1-基)丙烷-2-醇在化学治疗领域中作为降压药物非常有用。首选的成员包括在苯氧基上取代有乙酰胺甲基、羧甲基或氨甲酰甲基基团的化合物。还提供了其他制备方法。
• Alkanolamine derivatives
  申请人：Imperial Chemical Industries PLC

  公开号：US04419363A1

  公开（公告）日：1983-12-06

  Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.

  小说1-芳氧基-3-酰胺基烷基氨基-2-丙醇衍生物，其制造过程，包含它们的制药组合物以及在治疗心脏疾病中使用它们的方法。所披露的化合物的代表是1-(o-氰基苯氧基)-3-.beta.-(2-硫代乙酰胺基)乙基氨基丙醇。
• CH599924
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• CH614925
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