1-(2-羟基-3-苯氧基丙基)吡咯烷-2,5-二酮 | 83195-24-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 1-(2-羟基-3-苯氧基丙基)吡咯烷-2,5-二酮
• 英文名称: 1-(2-hydroxy-3-phenoxypropyl)pyrrolidine-2,5-dione
• 英文别名: N-(2-hydroxy-3-phenoxy-propyl)-succinimide；N-(2-Hydroxy-3-phenoxy-propyl)-succinimid；1-Succinimido-3-phenoxy-2-propanol；N-(2-Hydroxy-3-phenoxy-propyl)-succinimid
• CAS: 83195-24-8
• 化学式: C₁₃H₁₅NO₄
• 分子量: 249.266
• InChiKey: RQRSZRNJLQQNGJ-UHFFFAOYSA-N

物化性质

• 熔点：
  132 °C
• 沸点：
  491.3±35.0 °C(Predicted)
• 密度：
  1.290±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(2-羟基-3-苯氧基丙基)吡咯烷-2,5-二酮 在 chromium(VI) oxide 、 水 、 溶剂黄146 作用下， 生成 N-(2-oxo-3-phenoxy-propyl)-succinimide
  参考文献：
  名称：

  Anxiety, Cognitive Performance, and Cognitive Decline in Normal Aging

  摘要：

  A sample of 704 cognitively intact individuals (M age = 63.7 years) performed a battery of cognitive tests on as many as three occasions, at approximately 3-year intervals. The authors used random effects models to analyze cross-sectional relationships between cognitive performance and state anxiety and longitudinal relationships between cognitive change and neuroticism, after controlling for gender, age, and education. Cross-sectionally, higher state anxiety was associated with poorer performance on Wechsler Adult Intelligence Scale Synonyms, WIT III Analogies, Koh's Block Design, two measures of visual learning (Names and Faces and Thurstone's Picture Memory), and, for men, CVB-Scales Digit Span Test and Card Rotations. In longitudinal models, the main effects for neuroticism were significant for Block Design, Symbol Digit, and Names and Faces, but there were no significant interactions among neuroticism, gender, and time. These results provide some support for Eysenck's processing efficiency theory but none for neuroticism as a risk factor for cognitive decline in normal aging.

  DOI：

  10.1093/geronb/57.3.p246
• 作为产物：
  描述：

  丁二酰亚胺 、 苯基缩水甘油醚 在 吡啶 作用下， 以 乙醇 为溶剂， 反应 4.0h， 以72%的产率得到1-(2-羟基-3-苯氧基丙基)吡咯烷-2,5-二酮
  参考文献：
  名称：

  超短效β-肾上腺素受体阻断剂。1.在氮取代基中包含酯的（芳氧基）丙醇胺。

  摘要：

  为了产生短效的β-肾上腺素受体阻断剂，我们制备了几种具有酯官能团的（芳氧基）丙醇胺并入氮取代基。这些化合物中的许多在连续静脉输注40分钟后显示出很短的阻断活性。然而，发现它们的持续时间随着更长的静脉内输注而显着增加。

  DOI：

  10.1021/jm00354a002

文献信息

• Compounds and method for treatment or prophylaxis of cardiac disorders
  申请人：American Hospital Supply Corporation

  公开号：US04450173A1

  公开（公告）日：1984-05-22

  A short-acting .beta.-blocking compound of the formula ##STR1## wherein Ar may be substituted or unsubstituted aromatic, Y may be a straight or branched carbon chain or aralkyl, R may be lower alkyl, lower alkenyl, lower alkynyl, aryl or aralkyl, and x is an integer from 1 to about 3; or a pharmaceutically acceptable salt thereof.

  一种短效β-阻滞化合物的化学式为##STR1##其中Ar可能是取代或未取代的芳香族，Y可能是直链或支链碳链或芳基烷基，R可能是低碳链基，低烯基，低炔基，芳基或芳基烷基，x为1到约3之间的整数；或其药用盐。
• NOVEL DIPEPTIDYL-PEPTIDASE-IV INHIBITORS
  申请人：Li Weixing

  公开号：US20130184322A1

  公开（公告）日：2013-07-18

  The invention comprises novel inhibitors of dipeptidyl peptidase IV (DPP-IV) with beta blocker activity, pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP-IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP-IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, hypertension, and glaucoma of such other enumerated conditions as can be treated with inhibitors of DPP-IV and beta blockers.

  该发明涉及一种具有β受体阻滞剂活性的新型二肽基肽酶IV（DPP-IV）抑制剂，其中包括含有治疗有效量的新型DPP-IV抑制剂的药物组合物，以及治疗医学状况的新型方法。本文所述的新型DPP-IV抑制剂对于治疗神经系统疾病、糖尿病、炎症性疾病如关节炎、肥胖症、骨质疏松症、高血压和青光眼等其他已知的可以使用DPP-IV抑制剂和β受体阻滞剂治疗的疾病具有用处。
• Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension
  申请人：Yang Catherine

  公开号：US09115082B2

  公开（公告）日：2015-08-25

  The invention comprises novel inhibitors of dipeptidyl peptidase IV (DPP-IV) with beta blocker activity, pharmaceutical compositions comprising therapeutically effective amounts of novel inhibitors of DPP-IV, and novel methods of treating medical conditions are provided. The novel inhibitors of DPP-IV described herein are useful in the treatment of neurological disorders, diabetes, inflammatory disorders such as arthritis, obesity, osteoporosis, hypertension, and glaucoma of such other enumerated conditions as can be treated with inhibitors of DPP-IV and beta blockers.

  本发明涉及一种具有β受体阻滞剂活性的新型二肽基肽酶IV（DPP-IV）抑制剂，包括含有治疗有效量的新型DPP-IV抑制剂的制药组合物，以及治疗医疗状况的新型方法。本文所述的新型DPP-IV抑制剂对于治疗神经系统疾病、糖尿病、炎症性疾病如关节炎、肥胖症、骨质疏松症、高血压和青光眼等可使用DPP-IV抑制剂和β受体阻滞剂治疗的其他列举疾病都是有用的。
• Petrow; Stephenson, Journal of Pharmacy and Pharmacology, 1953, vol. 5, p. 359,366
  作者：Petrow、Stephenson

  DOI：——

  日期：——
• Zur Darstellung einiger Phenoxypropanolamine II. Mitteilung: Aminolyse von Epoxyden
  作者：Hermann J. Roth

  DOI：10.1002/ardp.19592920405

  日期：——