4-丙酰基-2-哌嗪酮 | 65493-55-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 4-丙酰基-2-哌嗪酮
• 英文名称: 4-Propanoylpiperazin-2-one
• CAS: 65493-55-2
• 化学式: C₇H₁₂N₂O₂
• mdl: MFCD17237618
• 分子量: 156.184
• InChiKey: HQUGNUJTASFXAK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.714
• 拓扑面积：
  49.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-丙酰基-2-哌嗪酮 、 苯甲酰氯 在 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 为溶剂， 反应 0.5h， 以30%的产率得到
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050
• 作为产物：
  描述：

  2-哌嗪酮 、 丙酸酐 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 0.5h， 以90%的产率得到4-丙酰基-2-哌嗪酮
  参考文献：
  名称：

  Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers

  摘要：

  A series of 2-oxopiperazine, 4-aminomethyl-, 3-amino- and 3-aminomethylpiperidine analogues of DM235 (sunifiram) and MN19 (sapunifiram), two previously reported potent cognition-enhancers, have been synthesized and tested in the mouse passive-avoidance test. The compounds display minimal effective doses in the range 0.3-10 mg/kg. Although the new substances do not show improved activity when compared to the parent compounds, some useful information has been obtained to understand structure-activity relationships. In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.050

文献信息

• [EN] SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY<br/>[FR] DIHYDROPYRIMIDINONES BICYCLIQUES SUBSTITUÉES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE L'ACTIVITÉ ÉLASTASE DE NEUTROPHILES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2014135414A1

  公开（公告）日：2014-09-12

  This invention relates to substituted bicyclic dihydropyrimidinones of formula (1) and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.

  这项发明涉及式（1）的取代双环二氢嘧啶酮及其作为中性粒细胞弹性蛋白酶活性抑制剂的用途，含有这些化合物的药物组合物，以及将其用作治疗和/或预防肺部、胃肠道和泌尿系统疾病、皮肤和眼睛的炎症性疾病以及其他自身免疫和过敏性疾病、移植物排斥反应和肿瘤性疾病的药剂的方法。
• Substituted Bicyclic Dihydropyrimidinones And Their Use As Inhibitors Of Neutrophil Elastase Activity
  申请人：GNAMM Christian

  公开号：US20140249129A1

  公开（公告）日：2014-09-04

  This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.

  这项发明涉及公式1的取代双环二氢嘧啶酮及其作为中性粒细胞弹性蛋白酶活性抑制剂的用途，包含这些化合物的药物组合物，以及将其用作治疗和/或预防肺部、胃肠道和泌尿系统疾病、皮肤和眼睛的炎症性疾病以及其他自身免疫和过敏性疾病、移植物排斥反应和肿瘤性疾病的方法。
• Piperidine derivative and use thereof
  申请人：Shirai Junya

  公开号：US20080275085A1

  公开（公告）日：2008-11-06

  The present invention provides a novel piperidine derivative and a tachykinin receptor antagonist containing same, as well as a compound represented by the formula: wherein R 1 is carbamoylmethyl, methylsulfonylethylcarbonyl and the like; R 2 is methyl or cyclopropyl; R 3 is a hydrogen atom or methyl; R 4 is a chlorine atom or trifluoromethyl; R 5 is a chlorine atom or trifluoromethyl; and a group represented by the formula: is a group represented by the formula: wherein R 6 is a hydrogen atom, methyl, ethyl or isopropyl; R 7 is a hydrogen atom, methyl or a chlorine atom; and R 8 is a hydrogen atom, a fluorine atom, a chlorine atom or methyl; or 3-methylthiophen-2-yl, and a salt thereof.

  本发明提供了一种新颖的哌啶衍生物和含有该衍生物的催吐肽受体拮抗剂，以及由下式表示的化合物： 其中R1为羰胺甲基、甲磺酰乙基羰基等；R2为甲基或环丙基；R3为氢原子或甲基；R4为氯原子或三氟甲基；R5为氯原子或三氟甲基；以及由下式表示的基团： 是由下式表示的基团： 其中R6为氢原子、甲基、乙基或异丙基；R7为氢原子、甲基或氯原子；R8为氢原子、氟原子、氯原子或甲基；或3-甲基噻吩-2-基，并且其盐。
• 3-(Carboxyethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
  申请人：Gruenenthal GmbH

  公开号：US20170197919A1

  公开（公告）日：2017-07-13

  The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diazaspiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

  这项发明涉及3-(羧乙基)-8-氨基-2-氧代-1,3-二氮杂螺[4.5]-癸烷衍生物，它们的制备以及它们在医学中的应用，特别是在疼痛治疗中的应用。
• SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
  申请人：GNAMM Christian

  公开号：US20140221335A1

  公开（公告）日：2014-08-07

  This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.

  该发明涉及式1的取代双环二氢嘧啶酮及其用作中性粒细胞弹性蛋白酶活性抑制剂的药物组合物，以及使用它们作为治疗和/或预防肺部、胃肠道和泌尿系统疾病、皮肤和眼部炎症性疾病、以及其他自身免疫和过敏性疾病、移植物排斥反应和肿瘤性疾病的药剂的方法。