tert-butyl 3-(3-methyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboxylate | 1121057-53-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: tert-butyl 3-(3-methyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboxylate
• CAS: 1121057-53-1
• 化学式: C₁₂H₁₉N₃O₃
• 分子量: 253.301
• InChiKey: JCOXIBYCDBFXNL-UHFFFAOYSA-N

物化性质

• 密度：
  1.169

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  68.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  1-BOC-吡咯烷-3-甲酸 、 N,N-二异丙基乙胺 、 O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate 、 N-羟基乙脒 在 乙酸乙酯 、 碳酸氢钠 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.5h， 以to give 3-(3-methyl-[1,2,4]oxadiazol-5-yl)-pyrrolidine-1-carboxylic acid tert-butyl ester as a yellow oil (192 mg)的产率得到tert-butyl 3-(3-methyl-1,2,4-oxadiazol-5-yl)pyrrolidine-1-carboxylate
  参考文献：
  名称：

  Certain Nitrogen Containing Bicyclic Chemical Entities For Treating Viral Infections

  摘要：

  提供了某些化学实体、制药组合物和治疗方法，用于治疗黄病毒科的成员，例如丙型肝炎病毒（丙肝或HCV）。

  公开号：

  US20120121540A1

文献信息

• [EN] PHENYL-3-AZA-BICYCLO[3.1.0]HEX-3-YL-METHANONES AND THE USE THEREOF AS MEDICAMENT<br/>[FR] PHÉNYL-3-AZA-BICYCLO[3.1.0]HEX-3-YL-MÉTHANONES ET LEUR UTILISATION EN TANT QUE MÉDICAMENT
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2013017657A1

  公开（公告）日：2013-02-07

  The present inventions relates to substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl- methanones of general formula (I) wherein R1, R2, R3, R4, R5 and R6 are as herein described or salts thereof, preferably pharmaceutically acceptable salts thereof. The invention further relates to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various conditions such as conditions concerning positive and negative symptoms of schizophrenia as well as cognitive impairments associated with schizophrenia, Alzheimers Disease and other neurological and psychiatric disorders. The compounds of the invention show glycine transporter-1 (GlyT1) inhibiting properties.

  本发明涉及通式（I）所示的取代苯基-3-氮杂双环[3.1.0]己-3-基甲酮，其中R1、R2、R3、R4、R5和R6如本文所述或其盐，优选为其药学上可接受的盐。本发明还涉及所述化合物的制备，包含符合通式（I）的化合物的药物组合物，以及利用所述化合物治疗各种疾病的用途，如涉及精神分裂症的阳性和阴性症状以及与精神分裂症、阿尔茨海默病和其他神经和精神障碍相关的认知障碍。本发明的化合物显示甘氨酸转运蛋白-1（GlyT1）抑制性能。
• [EN] COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR AMÉLIORER LA FONCTION COGNITIVE, PROCÉDÉS DE FABRICATION ET MÉTHODES DE TRAITEMENT
  申请人：MITHRIDION INC

  公开号：WO2010102218A1

  公开（公告）日：2010-09-10

  Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

  提供了用于刺激肌气受体并治疗认知障碍的肌气受体激动剂。还提供了合成这类激动剂的方法。还提供了用于增强人类等受试者认知功能的组合物，该组合物包括肌气受体激动剂或其药用适宜形式。还提供了通过给予这类组合物来治疗动物如人类的方法。
• [EN] COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING<br/>[FR] COMPOSÉS ET COMPOSITIONS POUR L'AMÉLIORATION DE LA COGNITION, LEURS PROCÉDÉS DE FABRICATION, ET MÉTHODES DE TRAITEMENT
  申请人：MITHRIDION INC

  公开号：WO2011085406A1

  公开（公告）日：2011-07-14

  Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.

  揭示了包括噻唑二唑衍生物在内的肌碱激动剂化合物，以及其组合物和制剂。还揭示了合成这种噻唑二唑化合物的方法。进一步揭示了使用这些肌碱激动剂或其药学适宜形式来增强认知功能的治疗方法。
• COMPOUNDS AND COMPOSITIONS FOR COGNITION-ENHANCEMENT, METHODS OF MAKING, AND METHODS OF TREATING
  申请人：Twose Trevor M.

  公开号：US20120046273A1

  公开（公告）日：2012-02-23

  Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.

  提供了用于刺激毒蕈碱受体和治疗认知障碍的毒蕈碱激动剂。还提供了合成这种激动剂的方法。还提供了用于增强人类等受试者认知功能的组合物，其中组合物包括毒蕈碱激动剂或其药学上适宜的形式。还提供了通过给予这样的组合物治疗人类等动物的方法。
• Cognition Enhancing Compounds and Compositions, Methods of Making, and Methods of Treating
  申请人：Mithridion, Inc.

  公开号：US20130274299A1

  公开（公告）日：2013-10-17

  The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.

  本发明涉及肌肉碱受体激动剂，其可用于刺激肌肉碱受体和治疗认知障碍。本文所披露的肌肉碱受体激动剂包括噁唑烷衍生物、组合物及其制备。还提供了合成噁唑烷化合物的方法。本公开还涉及用于增强人类等受试者认知功能的组合物，该组合物包括肌肉碱受体激动剂或其药学适宜形式。本公开还涉及通过给予该类组合物治疗动物，如人类的方法。