(+/-)-3-Ethyl-3-phenylpiperidin-2,6-dion | 2900-50-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (+/-)-3-Ethyl-3-phenylpiperidin-2,6-dion
• 英文别名: Glutarimide, 3-ethyl-3-phenyl-；4-ethyl-4-phenylpiperidine-2,6-dione
• CAS: 2900-50-7
• 化学式: C₁₃H₁₅NO₂
• 分子量: 217.268
• InChiKey: NSCAOEOKWMLESY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  46.2
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• [EN] 2,6-DIOXOPIPERIDINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
  申请人：NATIONAL RESEARCH DEVELOPMENT CORPORATION

  公开号：WO1985002618A1

  公开（公告）日：1985-06-20

  (EN) In the treatment of oestrogen-dependent tumours, it is desirable to improve the therapy obtainable from the compound aminoglutethimide. It has now been found that 3-ethyl-3-(4-pyridyl)glutarimide and derivatives thereof of formula (I), wherein R represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms offers advantages over aminoglutethimide. 3-Ethyl-3-(4-pyridyl)glutarimide can be prepared by various ring-closing reactions, especially by heating 4-(4-pyridyl)-hexano-1,4-dinitrile with a strong mineral acid.(FR) Dans le traitement des tumeurs dépendant des oestrogènes, il est désirable d'améliorer la thérapie que l'on peut pratiquer à l'aide du composé aminoglutéthimide. On a remarqué que le 3-éthyl-3-(4-pyridyl)glutarimide et ses dérivés de formule (I), où R représente un atome d'hydrogène ou un groupe alkyle possédant de 1 à 4 atomes de carbone, présentent des avantages par rapport à l'aminoglutéthimide. Le 3-éthyl-3-(4-pyridyl)glutarimide peut être préparé par plusieurs réactions à fermeture d'anneau, notamment en chauffant du 4-(4-pyridyl)-hexano-1,4-dinitrile avec un acide minéral fort.

  在治疗雌激素依赖性肿瘤时，改善从氨基戊酸咪唑化合物中获得的治疗效果是可取的。现在发现，式（I）中R代表氢原子或具有1到4个碳原子的烷基基团的3-乙基-3-（4-吡啶基）戊二酰亚胺及其衍生物比氨基戊酸咪唑具有优点。3-乙基-3-（4-吡啶基）戊二酰亚胺可以通过各种环闭合反应制备，特别是通过用强矿酸加热4-（4-吡啶基）-己二腈。
• Glutarimide derivatives, their preparation and pharmaceutical compositions containing them
  申请人：NATIONAL RESEARCH DEVELOPMENT CORPORATION

  公开号：EP0169062A1

  公开（公告）日：1986-01-22

  In the treatment of oestrogen-dependent tumours, it is desirable to improve the therapy obtainable from the compound aminoglutethimide. It has now been found that 3-ethyl-3-(4-pyridyl)glutarimide derivatives of formula wherein: (a) R' represents an ethyl group and R2 repsesents a methyl group, an alkyl or cycloalkyl group having 3 to 10 carbon atoms, or a fluoroalkyl group having 2 to 10 carbon atoms; (b) R represents an alkyl group having 3 to 10 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R2 represents a hydrogen atom; or, (c) R1 represents an alkyl group having 3 to 8 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R2 represents an alkyl or fluoroalkyl group having 2 to 8 carbon atoms, provided that the total number of carbon atoms in R1 and R2 is not more than 10; and therapeutically acceptable acid addition salts of the above compounds.

  在治疗雌激素依赖性肿瘤的过程中，希望能改善氨鲁米特化合物的治疗效果。现在发现，3-乙基-3-(4-吡啶基)戊二亚胺衍生物的式 式中 (a) R' 代表乙基，R2 代表甲基、具有 3 至 10 个碳原子的烷基或环烷基或具有 2 至 10 个碳原子的氟烷基； (b) R 代表具有 3 至 10 个碳原子的烷基或具有 2 至 5 个碳原子的氟烷基，R2 代表氢原子；或 (c) R1 代表具有 3 至 8 个碳原子的烷基或具有 2 至 5 个碳原子的氟烷基，R2 代表具有 2 至 8 个碳原子的烷基或氟烷基，条件是 R1 和 R2 中的碳原子总数不超过 10；以及上述化合物的治疗上可接受的酸加成盐。
• N-aryl-N-[4-(heterocyclicalkyl) piperidinyl]amides and pharmaceutical compositions and methods employing such compounds
  申请人：BOC, INC.

  公开号：EP0396282A2

  公开（公告）日：1990-11-07

  Novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, of the formula: including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein; R is selected from the group consisting of phenyl and substituted phenyl, wherein said substituents are members independently selected from halogen, lower-alkoxy, and combinations thereof; R₁ is a lower-alkyl group, lower-alkenyl group, or a lower-alkoxy lower alkyl having from 2 to 6 carbon atoms; R₂ is a heterocyclic lower-alkyl ring system selected from the group consisting of pyrrolyl lower-alkyl, pyrazolyl lower-alkyl, imidazolyl lower-alkyl, imidazolinyl lower-alkyl, imidazolyl lower-thioalkyl, triazolyl lower-alkyl, triazolyl lower-thioalkyl, tetrazolyl lower-alkyl, tetrazolyl lower-thioalkyl, thienyl lower-oxyalkyl, thienyl lower- hydroxyalkyl, thien-3-yl lower-alkyl, furanyl lower-hydroxyalkyl, thiazolyl lower-alkyl, oxazolyl lower-alkyl, thiadiazolyl lower-alkyl, oxadiazolyl lower-alkyl, piperidinyl loweralkyl, pyrimidinyl lower- alkyl, pyridazinyl lower-alkyl, triazinyl lower-alkyl, indolyl lower-alkyl, isoindolyl lower-alkyl, benzimidazolyl lower-alkyl, benzopyrazolyl lower-alkyl, benzoxazolyl lower-alkyl, benzopyranyl lower-alkyl, benzodioxanyl lower-alkyl, benzothiazinyl lower-alkyl, quinazolinyl lower-alkyl, purinyl lower-alkyl, phthalimidyl lower-alkyl, naphthalenecarboxamidyl lower-alkyl, and naphthalenesulfamidyl lower-alkyl; and R₃ is a member selected from the group consisting of hydrogen, lower-alkoxy carbonyl and lower-alkoxy methyl. R₄ is a hydrogen atom or a methyl group;

  可用作镇痛剂的新型取代 N-芳基-N-[4-(1-杂环烷基)哌啶基]酰胺，其式如下 包括光学活性异构体形式及其药学上可接受的酸加成盐，其中； R 选自苯基和取代苯基组成的组，其中所述取代基独立地选自卤素、低级烷氧基及其组合； R₁ 是具有 2 至 6 个碳原子的低级烷基、低级烯基或低级烷氧基； R₂ 是杂环低级烷基环系，选自由吡咯低级烷基、吡唑低级烷基、咪唑低级烷基、咪唑啉低级烷基、咪唑低级硫代烷基、三唑低级烷基组成的组、三唑基低硫代烷基、四唑基低烷基、四唑基低硫代烷基、噻吩基低氧代烷基、噻吩基低羟代烷基、噻吩-3-基低烷基、呋喃基低羟代烷基、噻唑基低烷基、噁唑基低烷基、噻二唑基低烷基、噁二唑低级烷基、哌啶低级烷基、嘧啶低级烷基、哒嗪低级烷基、三嗪低级烷基、吲哚低级烷基、异吲哚低级烷基、苯并咪唑低级烷基、苯并吡唑低级烷基、苯并恶唑低级烷基、低级烷基苯并吡喃基、低级烷基苯并二恶烷基、低级烷基苯并噻嗪基、低级烷基喹唑啉基、低级烷基嘌呤基、低级烷基邻苯二甲酰亚胺基、低级烷基萘甲酰胺基和低级烷基萘磺酰胺基；和 R₃ 选自氢、低级烷氧基羰基和低级烷氧基甲基组成的组。 R₄ 是氢原子或甲基；
• 2,6-Dioxopiperidine derivatives, their preparation and pharmaceutical compositions containing them
  申请人：NATIONAL RESEARCH DEVELOPMENT CORPORATION

  公开号：EP0147121B1

  公开（公告）日：1988-02-03
• US4668689A
  申请人：——

  公开号：US4668689A

  公开（公告）日：1987-05-26