1-Methyl-3-(phenylsulfonyl)pyrrolidine | 106368-98-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-Methyl-3-(phenylsulfonyl)pyrrolidine
• 英文别名: 3-(benzenesulfonyl)-1-methylpyrrolidine
• CAS: 106368-98-3
• 化学式: C₁₁H₁₅NO₂S
• 分子量: 225.312
• InChiKey: UOSZETBWCRGLCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  聚合甲醛 、 肌氨酸 、 苯基乙烯基砜 以 甲苯 为溶剂， 反应 0.25h， 以84%的产率得到1-Methyl-3-(phenylsulfonyl)pyrrolidine
  参考文献：
  名称：

  氨基酸方法作为不稳定偶氮次甲基叶立德的一般途径。轻松生成母体甲亚胺甲基化物及其 1-单取代和 1,1- 取代衍生物

  摘要：

  甘氨酸或 N-取代的甘氨酸与各种羰基化合物（如甲醛、芳香醛或酮）的脱羧缩合是获得母体甲基亚胺及其 1-单和 1,1-二取代衍生物的一种方便和通用的途径，有或没有N-取代基。

  DOI：

  10.1246/cl.1986.973

文献信息

• [EN] NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS<br/>[FR] COMPOSÉS AZOTÉS HÉTÉROCYCLIQUES CONVENANT COMME INHIBITEURS DE LA PDE10
  申请人：AMGEN INC

  公开号：WO2011143365A1

  公开（公告）日：2011-11-17

  Unsaturated nitrogen heterocyclic compounds of formula (I): (I), as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.

  式(I)的不饱和氮杂环化合物：(I)，如规范中定义的，含有它们的组合物，以及制备这种化合物的方法。本文还提供了通过抑制PDE10治疗可治疗的疾病或疾病的方法，如肥胖症、亨廷顿病、非胰岛素依赖型糖尿病、精神分裂症、躁郁症、强迫症等。
• Gonadotropin Releasing Hormone Receptor Antagonist, Preparation Method Thereof And Pharmaceutical Composition Comprising The Same
  申请人：Kim Seon Mi

  公开号：US20130137661A1

  公开（公告）日：2013-05-30

  Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

  披露了作为促性腺激素释放激素（“GnRH”）受体拮抗剂有用的化合物。
• Simple Generation of Nonstabilized Azomethine Ylides through Decarboxylative Condensation of α-Amino Acids with Carbonyl Compounds via 5-Oxazolidinone Intermediates
  作者：Otohiko Tsuge、Shuji Kanemasa、Masayuki Ohe、Shigeori Takenaka

  DOI：10.1246/bcsj.60.4079

  日期：1987.11

  Heating α-amino acids with a variety of carbonyl compounds generates N-unsubstituted or N-substituted azomethine ylides of nonstabilized types through the elimination of water and carbon dioxide. The ylides are captured by olefinic, acetylenic, and carbonyl dipolarophiles producing pyrrolidines, pyrrolines, and oxazolidines. The reaction involves intermediary 5-oxazolidinones which can be sometimes

  用各种羰基化合物加热 α-氨基酸，通过消除水和二氧化碳产生不稳定类型的 N-未取代或 N-取代的偶氮甲碱叶立德。叶立德被烯属、炔属和羰基亲偶极分子捕获，产生吡咯烷、吡咯啉和恶唑烷。该反应涉及有时可以分离的中间体 5-恶唑烷酮。母体偶氮甲碱叶立德的一些合成等价物，methaniminiummethylide，可通过该途径获得。
• AMINO ACID APPROACH AS A GENERAL ROUTE TO NONSTABILIZED AZOMETHINE YLIDES. FACILE GENERATION OF PARENT METHANIMINIUM METHYLIDE AND ITS 1-MONO- AND 1,1-DISUBSTITUTED DERIVATIVES
  作者：Otohiko Tsuge、Shuji Kanemasa、Masayuki Ohe、Shigeori Takenaka

  DOI：10.1246/cl.1986.973

  日期：1986.6.5

  condensation of glycine or N-substituted glycines with a variety of carbonyl compounds such as formaldehyde, aromatic aldehyde, or ketones is a convenient and general route to parent methaniminium methylide and its 1-mono- and 1,1-disubstituted derivatives with or without an N-substituent.

  甘氨酸或 N-取代的甘氨酸与各种羰基化合物（如甲醛、芳香醛或酮）的脱羧缩合是获得母体甲基亚胺及其 1-单和 1,1-二取代衍生物的一种方便和通用的途径，有或没有N-取代基。
• 2,4,6-TRIAMINO-1,3,5-TRIAZINE DERIVATIVE
  申请人：Kubota Hideki

  公开号：US20080227785A1

  公开（公告）日：2008-09-18

  This invention relates to an anti-dementia agent which uses a BEC 1 potassium channel inhibitor as the active ingredient. It was proved that the BEC 1 potassium channel inhibitor has an action to improve learning disorder and is useful as a preventive or therapeutic agent for diseases, preferably dementia, in which the BEC 1 potassium channel is considered to be concerned. Illustratively, it was confirmed by an in vivo test that the BEC 1 potassium channel inhibitor has an action to improve learning disorder. Also, it was found that a compound having 2,4,6-triamino-1,3,5-triazine has a BEC 1 potassium channel inhibitory action.

  本发明涉及一种以BEC 1钾离子通道抑制剂作为活性成分的抗痴呆剂。已经证明，BEC 1钾离子通道抑制剂具有改善学习障碍的作用，并且作为预防或治疗剂是有用的，尤其是对于BEC 1钾离子通道与之相关的疾病，如痴呆症。例如，通过体内试验证实，BEC 1钾离子通道抑制剂具有改善学习障碍的作用。此外，还发现具有2,4,6-三氨基-1,3,5-三嗪的化合物具有BEC 1钾离子通道抑制作用。