N-[(1-benzoyloxyethoxy)carbonyloxy]succinimide | 918448-41-6

• 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: N-[(1-benzoyloxyethoxy)carbonyloxy]succinimide
• 英文别名: 1-((((2,5-Dioxopyrrolidin-1-yl)oxy)carbonyl)oxy)ethyl benzoate；1-(2,5-dioxopyrrolidin-1-yl)oxycarbonyloxyethyl benzoate
• CAS: 918448-41-6
• 化学式: C₁₄H₁₃NO₇
• 分子量: 307.26
• InChiKey: LALJUOXHFMKATO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  99.2
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  tranexamic acid 、 N-[(1-benzoyloxyethoxy)carbonyloxy]succinimide 以 MTBE acetone water 为溶剂， 以to yield the title compound 23 (160 mg, 18% yield) as a white powder的产率得到trans-4-{[1-(benzoyloxy)ethoxycarbonyl]aminomethyl}-cyclohexanecarboxylic acid
  参考文献：
  名称：

  ACYLOXYALKYL CARBAMATE PRODRUGS OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE

  摘要：

  本文公开了trans-4-（氨甲基）-环己烷羧酸的酰氧基烷基氨基甲酸酯前药、其制药组合物、制备trans-4-（氨甲基）-环己烷羧酸酯前药的方法，以及使用trans-4-（氨甲基）-环己烷羧酸酯前药和制药组合物治疗或预防各种疾病或障碍的方法。本文还公开了适用于口服、局部使用和使用缓释剂型的酰氧基烷基氨基甲酸酯前药和制药组合物。

  公开号：

  US20080153898A1

文献信息

• Acyloxyalkyl carbamate prodrugs of alpha-amino acids, methods of synthesis and use
  申请人：Dai Xuedong

  公开号：US20080051458A1

  公开（公告）日：2008-02-28

  Acyloxyalkyl carbamate prodrugs of α-amino acids, pharmaceutical compositions thereof, methods of making acyloxyalkyl carbamate prodrugs of α-amino acids and methods of using acyloxyalkyl carbamate prodrugs of α-amino acids, and pharmaceutical compositions thereof to treat a disease are disclosed. Acyloxyalkyl carbamate prodrugs of α-amino acids suitable for oral administration using sustained release dosage forms are also disclosed.

  本发明公开了α-氨基酸的酰氧基烷基氨基甲酸酯前药、其制药组合物、制备酰氧基烷基氨基甲酸酯前药的方法以及使用酰氧基烷基氨基甲酸酯前药和其制药组合物治疗疾病的方法。本发明还公开了适用于口服缓释剂型的α-氨基酸的酰氧基烷基氨基甲酸酯前药。
• Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use
  申请人：Zerangue Noa

  公开号：US20070027210A1

  公开（公告）日：2007-02-01

  Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

  本发明公开了trans-4-(aminomethyl)-环己烷羧酸的酰氧基烷基氨基甲酸酯前药、其制药组合物、制备trans-4-(aminomethyl)-环己烷羧酸酯类前药的方法，以及使用trans-4-(aminomethyl)-环己烷羧酸酯类前药和制药组合物来治疗或预防各种疾病或紊乱的方法。本发明还公开了适用于口服、局部应用以及使用持续释放剂型给药的酰氧基烷基氨基甲酸酯前药和制药组合物。
• Acyloxyalkyl Carbamate Prodrugs of Tranexamic Acid, Methods of Synthesis and Use
  申请人：Zerangue Noa

  公开号：US20100036148A1

  公开（公告）日：2010-02-11

  Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid, pharmaceutical compositions thereof, methods of making prodrugs of trans-4-(aminomethyl)-cyclohexane-carboxylic acid, and methods of using prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof to treat or prevent various diseases or disorders are disclosed. Acyloxyalkyl carbamate prodrugs of trans-4-(aminomethyl)-cyclohexanecarboxylic acid and pharmaceutical compositions thereof suitable for oral and topical administration and for administration using sustained release dosage forms are also disclosed.

  本发明公开了转-4-(氨甲基)-环己烷羧酸的酰氧基烷基氨基甲酸酯前药，其制药组合物，制备转-4-(氨甲基)-环己烷羧酸前药的方法，以及使用转-4-(氨甲基)-环己烷羧酸前药及其制药组合物治疗或预防各种疾病或疾患的方法。本发明还公开了适用于口服和局部给药以及使用持续释放剂量形式给药的转-4-(氨甲基)-环己烷羧酸的酰氧基烷基氨基甲酸酯前药和其制药组合物。
• Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
  申请人：Gallop Mark A.

  公开号：US20080146526A1

  公开（公告）日：2008-06-19

  Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

  本发明揭示了3-氨基丙基膦酸及其类似物的酰氧基烷基氨基甲酸酯前药，制备酰氧基烷基氨基甲酸酯前药的方法，使用酰氧基烷基氨基甲酸酯前药的方法，以及包含酰氧基烷基氨基甲酸酯前药的制药组合物，用于治疗轻度认知障碍、与阿尔茨海默病相关的认知障碍、抑郁症、焦虑症和癫痫等疾病或疾病。本发明还揭示了适用于口服和持续释放口服剂型的3-氨基丙基膦酸及其类似物的酰氧基烷基氨基甲酸酯前药。
• ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE
  申请人：Gallop Mark A

  公开号：US20090286759A1

  公开（公告）日：2009-11-19

  Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

  本发明涉及3-氨基丙基膦酸及其类似物的酰氧基烷基氨基甲酸酯前药，制备酰氧基烷基氨基甲酸酯前药的方法，使用酰氧基烷基氨基甲酸酯前药的方法，以及包含酰氧基烷基氨基甲酸酯前药的制药组合物，用于治疗轻度认知障碍、与阿尔茨海默病相关的认知障碍、抑郁症、焦虑症和癫痫等疾病或疾病。本发明还涉及适用于口服和持续释放口服剂型的3-氨基丙基膦酸及其类似物的酰氧基烷基氨基甲酸酯前药。