1-acetoxy-3-carbamoyl-2,2,5,5-tetramethylpyrrolidine

• 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-acetoxy-3-carbamoyl-2,2,5,5-tetramethylpyrrolidine
• 英文别名: (3-carbamoyl-2,2,5,5-tetramethylpyrrolidin-1-yl) acetate
• 化学式: C₁₁H₂₀N₂O₃
• 分子量: 228.291
• InChiKey: YOGFCZDXOYHHJN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  72.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-hydroxy-3-carbamoyl-2,2,5,5-tetramethylpyrrolidine 在 乙酸酐 、 碳酸氢钠 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 以86%的产率得到1-acetoxy-3-carbamoyl-2,2,5,5-tetramethylpyrrolidine
  参考文献：
  名称：

  EP1132085

  摘要：

  公开号：

文献信息

• N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor
  申请人：Daiichi Radioisotope Laboratories, Ltd.

  公开号：US06713492B1

  公开（公告）日：2004-03-30

  Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

  含有N-酰氧化环烷基化合物的药物或试剂，所述化合物的活性成分由通式（I）表示：其中A是可选取代的C4或C5环烷基，环中可能有一个双键；R是C1-C3烷基或苯基。上述化合物是羟胺衍生物，作为自旋捕获剂，可以快速与自由基或活性氧在目标器官中反应，尽管它们在制备或给药期间稳定性优异。
• Sensitive ESR Determination of Intracellular Oxidative Stress by Using Acyl-Protected Hydroxylamines as New Spin Reagents
  作者：Osamu Itoh、Masaaki Aoyama、Hidekatsu Yokoyama、Heitaro Obara、Hiroaki Ohya、Hitoshi Kamada

  DOI：10.1246/cl.2000.304

  日期：2000.4

  Several acyl-protected hydroxylamines were synthesized as new spin reagents for ESR measurements of intracellular oxidative stress. These compounds were stable non-radical compounds, but were easily deprotected with esterase to yield hydroxylamines, which were oxidized by oxidants to yield ESR- detectable nitroxide radical. Using an acyl-protected hydroxylamine, a highly sensitive ESR determination procedure was successfully conducted to analyze oxidative stress in human leukocytes.

  我们合成了几种酰基保护的羟胺，作为 ESR 测量细胞内氧化应激的新自旋试剂。这些化合物是稳定的非自由基化合物，但很容易用酯酶进行脱保护，生成羟胺，羟胺被氧化剂氧化后生成 ESR 可检测到的亚硝基自由基。利用酰基保护的羟胺，成功地进行了高灵敏度的 ESR 测定程序，以分析人类白细胞中的氧化应激。
• DRUGS AND REAGENTS CONTAINING N-ACYLOXYLATED CYCLOALKYL COMPOUNDS AS THE ACTIVE INGREDIENT
  申请人：DAIICHI RADIOISOTOPE LABORATORIES, LTD.

  公开号：EP1132085A1

  公开（公告）日：2001-09-12

  Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): (wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1 - C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

  含有通式（I）代表的 N-酰氧基化环烷基化合物作为活性成分的药物或试剂：（其中 A 是任选取代的 C4 或 C5 环烷基，环中可能有一个双键；R 是 C1 - C3 烷基或苯基）。 上述化合物是羟胺衍生物，具有自旋捕获剂的功能，尽管在制备或给药过程中具有极佳的稳定性，但在客观器官中会迅速与自由基或活性氧发生反应。
• US6713492B1
  申请人：——

  公开号：US6713492B1

  公开（公告）日：2004-03-30