1-癸酰基-2-吡咯烷酮 | 33602-03-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 1-癸酰基-2-吡咯烷酮
• 英文名称: 1-decanoyl-2-pyrrolidinone
• 英文别名: 2-Pyrrolidinone, 1-(1-oxodecyl)-；1-decanoylpyrrolidin-2-one
• CAS: 33602-03-8
• 化学式: C₁₄H₂₅NO₂
• 分子量: 239.358
• InChiKey: ZWIZLSQLKQJUQT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  17
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-(吡咯烷-1-基)癸-1-酮 在 CrO₃-3.5-dimethylpyrazole 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以81%的产率得到1-癸酰基-2-吡咯烷酮
  参考文献：
  名称：

  Oxidation of N-Acyl-pyrrolidones to Imides with CrO3·3,5-dimethylpyrazole

  摘要：

  N-Acyl-pyrrolidones are easily obtained by treatment of N-acyl-pyrrolidines with CrO3 . 3,5-dimethylpyrazole complex (CrO3 . 3,5-DMP) at room temperature. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0040-4039(97)10161-7

文献信息

• Verfahren zur Herstellung von Amidoperoxicarbonsäuren
  申请人：HOECHST AKTIENGESELLSCHAFT

  公开号：EP0739880A2

  公开（公告）日：1996-10-30

  Verfahren zur Herstellung von Amidoperoxicarbonsäuren umfassend die Verfahrensschritte: Ringöffnung des N-Acyllactams zu der entsprechenden Amidocarbonsäure und nachfolgend Oxidation der erhaltenen Amidocarbonsäure zur entsprechenden Amidoperoxicarbonsäure.

  制备脒基过氧羧酸的工艺，包括以下步骤：N-酰基内酰胺开环生成相应的脒基羧酸，然后将生成的脒基羧酸氧化成相应的脒基过氧羧酸。
• Alprostadil alkyl ester-containing composition for external application
  申请人：WHAN IN PHARM. CO., LTD.

  公开号：US20030125382A1

  公开（公告）日：2003-07-03

  The present invention relates to a composition of topical preparation containing alprostadil alkyl ester, and more particularly, comprising an alprostadil alkyl ester, an oily vehicle, a skin permeation enhancer and an anti-irritant agent.

  本发明涉及一种含有阿洛前列地尔烷基酯的外用制剂组合物，特别是由阿洛前列地尔烷基酯、油性载体、皮肤渗透促进剂和抗刺激剂组成。
• [DE] VERWENDUNG VON N-ACYL-LACTAMEN ALS KRISTALLISATIONSINHIBITOREN<br/>[EN] USE OF N-ACYL LACTAMS AS CRYSTALLISATION INHIBITORS<br/>[FR] UTILISATION DE N-ACYLLACTAMES COMME INHIBITEURS DE LA CRISTALLISATION
  申请人：BAYER AKTIENGESELLSCHAFT

  公开号：WO1995019708A1

  公开（公告）日：1995-07-27

  (DE) N-Acyl-lactame der Formel (I), in welcher A und R die in der Beschreibung angegebenen Bedeutungen haben, lassen sich verwenden, um beim Ausbringen von wäßrigen Spritzbrühen, die A) bestimmte zur Kristallisation neigende Azol-Derivate und B) gegebenenfalls einen oder mehrere weitere Wirkstoffe sowie Zusatzstoffe enthalten, eine Kristallisation dieser zur Kristallisation neigenden Wirkstoffe in den Spritzgeräten zu verhindern.(EN) N-acyl lactams of formula (I), in which A and R have the meaning given in the description, may be used, when spraying aqueous spraying compounds containing A) certain crystallisation-prone azol derivatives and B) possibly one or more other active agents and additives, to prevent the crystallisation of such crystallisation-prone active agents in the spraying equipement.(FR) On peut utiliser des N-acyllactames de formule (I), dans laquelle A et R ont la signification indiquée dans la description, pour empêcher, lors de la pulvérisation de bouillies aqueuses contenant A) certains dérivés azoles ayant tendance à cristalliser et B) le cas échéant une ou plusieurs autres substances actives ainsi que des additifs, une cristallisation, dans les pulvérisateurs, de ces substances actives ayant tendance à cristalliser.

  (N-酰etyl化合物的结构式为 (I)，其中 A 和 R 表示该说明中所述的含义，可以通过喷水悬浮剂的方式使用，特别是喷水悬浮剂中含有以下两种成分或多种成分：A) 特定的晶核促进的尿素衍生物，和B) 可能含有一个或多个其他活性成分和添加剂。从而防止此类活性成分在喷水悬浮剂喷嘴中的结晶化 )。
• Synthesis and anticonvulsant activity of 1-acyl-2-pyrrolidinone derivatives
  作者：Hitoshi Sasaki、Yoshiyuki Mori、Junzo Nakamura、Juichiro Shibasaki

  DOI：10.1021/jm00106a025

  日期：1991.2

  Several 1-acyl-2-pyrrolidinone derivatives were synthesized as derivatives of gamma-aminobutyric acid (GABA), and their pharmacological activities and stabilities were investigated. The derivatives showed anticonvulsant effect on picrotoxin-induced seizure at a dose of 200 mg/kg. In particular, 1-decanoyl-2-pyrrolidinone (7) and 1-dodecanoyl-2-pyrrolidinone (8) had a high activity. The anticonvulsant activity showed a dose dependency. Some of 1-acyl-2-pyrrolidinone derivatives prolonged sleeping time which was induced by sodium pentobarbital and showed a recovery from disruption of the memory of passive avoidance response, which was induced by an electroconvulsive shock. As shown by the results of the stability study of 1-acetyl-2-pyrrolidinone (1), it was degraded in an acidic buffer and an alkaline buffer although 2-pyrrolidinone was stable. 1-Acyl-2-pyrrolidinone derivatives were degraded in liver and brain homogenates of mouse and rat. They showed a degradation rate in rat plasma. Conversion of 8 to GABA in mouse liver homogenate was demonstrated. These results suggested that the pharmacological activity of 1-acyl-2-pyrrolidinone is probably due to the release of GABA by hydrolysis of derivatives although further work is necessary.
• SASAKI, HITOSHI;MORI, YOSHIYKI;NAKAMURA, JUNZO;SHIBASAKI, JUICHIRO, J. MED. CHEM., 34,(1991) N, C. 628-633
  作者：SASAKI, HITOSHI、MORI, YOSHIYKI、NAKAMURA, JUNZO、SHIBASAKI, JUICHIRO

  DOI：——

  日期：——