1-((((2,5-dioxopyrrolidin-1-yl)oxy)carbonyl)oxy)-2-methylpropyl pivalate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 1-((((2,5-dioxopyrrolidin-1-yl)oxy)carbonyl)oxy)-2-methylpropyl pivalate
• 英文别名: 1-({[(2,5-dioxopyrrolidin-1-yl)oxy]carbonyl}oxy)-2-methylpropyl 2,2-dimethylpropanoate；1-[(2,5-Dioxopyrrolidinyl)oxycarbonyloxy]-2-methylpropyl 2,2-dimethylpropanoate；[1-(2,5-dioxopyrrolidin-1-yl)oxycarbonyloxy-2-methylpropyl] 2,2-dimethylpropanoate
• 化学式: C₁₄H₂₁NO₇
• 分子量: 315.323
• InChiKey: XCHBFYVHJGOFGL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  22
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.71
• 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：

  1-((((2,5-dioxopyrrolidin-1-yl)oxy)carbonyl)oxy)-2-methylpropyl pivalate 、 (R)-巴氯芬 在 碳酸氢钠 、 盐酸 作用下， 以 水 、 乙腈 为溶剂， 反应 1.0h， 生成 (3R)-3-(4-chlorophenyl)-4-[[1-(2,2-dimethylpropanoyloxy)-2-methylpropoxy]carbonylamino]butanoic acid
  参考文献：
  名称：

  [EN] ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE
  [FR] PRODROGUES A BASE DE CARBAMATE D'ALKYLE ACYLE, PROCEDE DE SYNTHESE ET UTILISATION

  摘要：

  公开号：

  WO2005019163A3
• 作为产物：
  描述：

  1-氯-2-甲基氯甲酸甲酯 在 过氧乙酸 、 三乙胺 、 N,N-二异丙基乙胺 作用下， 以 乙醚 、 二氯甲烷 、 溶剂黄146 为溶剂， 反应 96.17h， 生成 1-((((2,5-dioxopyrrolidin-1-yl)oxy)carbonyl)oxy)-2-methylpropyl pivalate
  参考文献：
  名称：

  [EN] PRODRUGS OF GLUTAMINE ANALOGS
  [FR] PROMÉDICAMENTS D'ANALOGUES DE GLUTAMINE

  摘要：

  公开号：

  WO2017023774A9

文献信息

• ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS
  申请人：Gallop Mark A.

  公开号：US20090234138A1

  公开（公告）日：2009-09-17

  The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

  本文披露了关于(±)-4-氨基-3-(4-氯苯基)丁酸及其类似物的酰氧基烷基氨基甲酸酯前药、其制药组合物、制备(±)-4-氨基-3-(4-氯苯基)丁酸及其类似物的前药的方法、使用(±)-4-氨基-3-(4-氯苯基)丁酸及其类似物的前药的方法，以及用于治疗或预防普通疾病和/或紊乱，如痉挛和/或酸反流病的制药组合物。本文还涉及适用于口服的(±)-4-氨基-3-(4-氯苯基)丁酸及其类似物的酰氧基烷基氨基甲酸酯前药以及其持续释放口服剂型。
• ACYLOXYALKYL CARBAMATE PRODRUGS, METHODS OF SYNTHESIS AND USE
  申请人：Gallop A. Mark

  公开号：US20080096960A1

  公开（公告）日：2008-04-24

  The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.

  本文涉及到(±)-4-氨基-3-(4-氯苯基)丁酸和其类似物的酰氧基烷基氨基甲酸酯前药、其制药组合物、制备(±)-4-氨基-3-(4-氯苯基)丁酸和其类似物的前药的方法、使用(±)-4-氨基-3-(4-氯苯基)丁酸和其类似物的前药的方法，以及其制药组合物用于治疗或预防常见疾病和/或疾病，如痉挛和/或酸逆流病。本文还涉及适用于口服的酰氧基烷基氨基甲酸酯前药和其持续释放口服剂型。
• 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 OF TRANEXAMIC ACID, METHODS OF SYNTHESIS AND USE
  申请人：Zerangue Noa

  公开号：US20080153898A1

  公开（公告）日：2008-06-26

  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。