(S)-1-methyl-2-(anilinomethyl)pyrrolidine | 82160-06-3

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (S)-1-methyl-2-(anilinomethyl)pyrrolidine
• 英文别名: N-[[(2S)-1-methylpyrrolidin-2-yl]methyl]aniline
• CAS: 82160-06-3
• 化学式: C₁₂H₁₈N₂
• 分子量: 190.288
• InChiKey: PSQSNNZIHWLLEC-LBPRGKRZSA-N

物化性质

• 沸点：
  301.5±15.0 °C(Predicted)
• 密度：
  1.030±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  15.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (S)-1-methyl-2-(anilinomethyl)pyrrolidine 、 苯甲醛 以66%的产率得到
  参考文献：
  名称：

  MUKAIYAMA, TERUAKI;IWASAWA, NOBUHARU;STEVENS, R. W.;HAGA, TORU, TETRAHEDRON, 1984, 40, N 8, 1381-1390

  摘要：

  DOI：
• 作为产物：
  描述：

  N(N-benzyloxycarbonylprolyl)aniline 在 lithium aluminium tetrahydride 作用下， 生成 (S)-1-methyl-2-(anilinomethyl)pyrrolidine
  参考文献：
  名称：

  N-亚苄基-DL-苯丙氨酸甲酯在手性锂酰胺存在下的对映体分化甲基化

  摘要：

  N-亚苄基-DL-苯丙氨酸甲酯的不对称甲基化在衍生自(S)-脯氨酸的仲胺的锂盐存在下进行。类似地使用聚（亚氨基-1-异丁基乙烯）的氨基化锂及其相应的低分子量模型化合物，衍生自（S）-亮氨酸，以检查聚合物对立体选择性的影响。

  DOI：

  10.1246/bcsj.55.961

文献信息

• Oxopyrrolidine compounds, preparation of said compounds and their use in the manufacturing of Levetiracetam and analogues
  申请人：Ates Celal

  公开号：US20060258734A1

  公开（公告）日：2006-11-16

  The present invention relates to an improved process for the preparation of (S)-(−)-α-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof. The invention also relates to compounds of the general formula (6) wherein R 1 is methyl or ethyl; and R 2 is C?2#191 -C?4#191 alkyl, C?2#191-C?4#191 alkenyl or C?2#191-C?4#191 alkynyl, optionally substituted by one or more halogen, and their preparation processes.

  本发明涉及一种改进的制备(S)-(-)-α-乙基-2-氧代-1-吡咯烷酰胺及其类似物的方法。该发明还涉及一般式(6)中R1为甲基或乙基; R2为C2-C4烷基、C2-C4烯基或C2-C4炔基，可以选择性地被一个或多个卤素取代，以及它们的制备方法。
• Oxopyrrolidine compounds, preparations of said compounds and their use in the manufacturing of levetiracetam and analogues
  申请人：——

  公开号：US20040204476A1

  公开（公告）日：2004-10-14

  The present invention relates to an improved process for the preparation of (S)-(−)-&agr;-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof. The invention also relates to compounds of the general formula (6) wherein R 1 is methyl or ethyl; and R 2 is C?2#19 1-C?4#191 alkyl, C?2#191 -C?4#191 alkenyl or C?2#191-C?4#191 alkynyl, optionally substituted by one or more halogen, and their preparation processes. 1

  本发明涉及一种改进的方法，用于制备(S)-(−)-α-乙基-2-氧代-1-吡咯烷乙酰胺及其类似物。本发明还涉及一般式（6）的化合物，其中R1为甲基或乙基；R2为C2-19的1-C4-191烷基、C2-191-C4-191烯基或C2-191-C4-191炔基，可选择地被一个或多个卤素取代，以及它们的制备方法。
• Oxopyrrolidine compounds, preparation of said compounds and their use in the manufacturing of levetiracetam and analogues
  申请人：Ates Celal

  公开号：US20070142647A1

  公开（公告）日：2007-06-21

  The present invention relates to an improved process for the preparation of (S)-(-)-α-ethyl-2-oxo-1-pyrrolidine acetamide and analogues thereof. The invention also relates to compounds of the general formula (6) wherein R 1 is methyl or ethyl; and R 2 is C 2 -C 4 alkyl, C 2 -C 4 alkenyl or C 2 -C 4 alkynyl, optionally substituted by one or more halogen, and their preparation processes.

  本发明涉及一种改进的方法，用于制备（S）-（-）-α-乙基-2-氧代-1-吡咯烷乙酰胺及其类似物。本发明还涉及一般式（6）中化合物的制备方法，其中R1为甲基或乙基; R2为C2-C4烷基，C2-C4烯基或C2-C4炔基，可以选择性地被一个或多个卤素取代。
• Novel Heterocyclic Substituted Carbonyl Derivatives and Their Use as Dopamine D3 Receptor Ligands
  申请人：Hendrix James A.

  公开号：US20090247509A1

  公开（公告）日：2009-10-01

  The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D 3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D 3 receptors.

  本发明涉及杂环取代羰基衍生物，其表现出对多巴胺D3受体的选择性结合。另一方面，本发明涉及一种治疗与多巴胺D3受体活性相关的中枢神经系统疾病的方法，该方法包括向需要此类治疗的患者施用所述化合物的治疗有效量，以缓解此类疾病。这些化合物可以治疗的中枢神经系统疾病包括精神疾病、物质依赖、物质滥用、运动障碍（例如帕金森病、帕金森综合症、神经阻滞引起的迟发性运动障碍、吉尔斯-德-拉-图雷综合症和亨廷顿病）、痴呆、焦虑症、睡眠障碍、昼夜节律紊乱和情绪障碍。本发明还涉及制备所述化合物的方法以及将所述化合物作为多巴胺D3受体成像剂的制备和使用方法。
• Novel heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands
  申请人：Hendrix A. James

  公开号：US20070161641A1

  公开（公告）日：2007-07-12

  The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates is to a method for treating central nervous system disorders associated with the dopamine D 3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D 3 receptors.

  本发明涉及杂环取代羰基衍生物，其具有选择性地与多巴胺D3受体结合。另一方面，本发明涉及一种治疗中枢神经系统疾病的方法，该疾病与多巴胺D3受体活性有关，包括对患者进行治疗，向患者施用所述化合物的治疗有效量，以缓解此类疾病。这些化合物可以治疗的中枢神经系统疾病包括精神病性障碍、物质依赖、物质滥用、运动障碍（例如帕金森病、帕金森综合症、神经阻滞剂引起的迟发性运动障碍、吉尔·德·拉·图雷特综合症和亨廷顿病）、痴呆、焦虑症、睡眠障碍、昼夜节律紊乱和情绪障碍。本发明还涉及所述化合物的制备过程，以及将所述化合物作为多巴胺D3受体成像剂的制备和使用方法。