3-cyclooctyl-7-(o-tolyl)thieno[3,2-d]pyrimidin-4(3H)-one | 1621979-93-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并嘧啶酮衍生物
• 英文名称: 3-cyclooctyl-7-(o-tolyl)thieno[3,2-d]pyrimidin-4(3H)-one
• 英文别名: 3-Cyclooctyl-7-(o-tolyl)thieno[3,2-d]pyrimidin-4(3H)-one；3-cyclooctyl-7-(2-methylphenyl)thieno[3,2-d]pyrimidin-4-one
• CAS: 1621979-93-8
• 化学式: C₂₁H₂₄N₂OS
• 分子量: 352.5
• InChiKey: ZHYZNEAKIGAXDO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.8
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  60.9
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3,7-diphenylthieno[3,2-d]pyrimidin-4(3H)-one 、 methyl 3-amino-4-(o-tolyl)thiophene-2-carboxylate 、 原甲酸三乙酯 、 环辛胺 以 溶剂黄146 为溶剂， 以to give 85.4 mg (0.24 mmol, 60.6% yield) of the title compound的产率得到3-cyclooctyl-7-(o-tolyl)thieno[3,2-d]pyrimidin-4(3H)-one
  参考文献：
  名称：

  THIENOPYRIMIDINONE DERIVATIVES AS mGluR1 ANTAGONISTS

  摘要：

  公开了一种作用于代谢型谷氨酸受体亚型1的拮抗剂噻吩嘧啶酮衍生物。噻吩嘧啶酮衍生物对代谢型谷氨酸受体相关疾病具有药理活性，包括疼痛，如神经病性疼痛和偏头痛，精神疾病，如焦虑症和精神分裂症，尿失禁以及神经退行性疾病，如帕金森病和阿尔茨海默病。还公开了制备噻吩嘧啶酮衍生物的方法，以及包含噻吩嘧啶酮衍生物作为活性成分的制药组合物。

  公开号：

  US20140228565A1

文献信息

• Thienopyrimidinone derivatives as mGluR1 antagonists
  申请人：KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

  公开号：US09260448B2

  公开（公告）日：2016-02-16

  Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

  本发明涉及噻唑嘧啶酮衍生物，作为代谢型谷氨酸受体亚型1的拮抗剂。该噻唑嘧啶酮衍生物对代谢型谷氨酸受体相关疾病具有药理活性，包括疼痛，如神经病性疼痛和偏头痛，精神疾病，如焦虑症和精神分裂症，尿失禁以及神经退行性疾病，如帕金森病和阿尔茨海默病。本发明还涉及制备噻唑嘧啶酮衍生物的方法，以及含有该噻唑嘧啶酮衍生物作为活性成分的药物组合物。
• US9260448B2
  申请人：——

  公开号：US9260448B2

  公开（公告）日：2016-02-16
• THIENOPYRIMIDINONE DERIVATIVES AS mGluR1 ANTAGONISTS
  申请人：KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY

  公开号：US20140228565A1

  公开（公告）日：2014-08-14

  Disclosed are thienopyrimidinone derivatives as antagonists that act on metabotropic glutamate receptor subtype 1. The thienopyrimidinone derivatives show pharmacological activity against metabotropic glutamate receptor-related diseases, including pain, such as neuropathic pain and migraine, psychiatric diseases, such as anxiety disorder and schizophrenia, urinary incontinence, and neurodegenerative diseases, such as Parkinson's disease and Alzheimer's disease. Also disclosed are methods for preparing the thienopyrimidinone derivatives, and pharmaceutical compositions containing the thienopyrimidinone derivatives as active ingredients.

  披露了作为对代谢型谷氨酸受体亚型1起作用的拮抗剂的噻吩嘧啶酮衍生物。这些噻吩嘧啶酮衍生物显示出对代谢型谷氨酸受体相关疾病的药理活性，包括疼痛，如神经病性疼痛和偏头痛，精神疾病，如焦虑症和精神分裂症，尿失禁，以及神经退行性疾病，如帕金森病和阿尔茨海默病。还披露了制备这些噻吩嘧啶酮衍生物的方法，以及含有这些噻吩嘧啶酮衍生物作为活性成分的药物组合物。