3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine | 625099-23-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine
• CAS: 625099-23-2
• 化学式: C₉H₉F₃N₂O
• 分子量: 218.178
• InChiKey: QDAFWNIVIJKEAB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  phenyl-[3-(trifluoromethoxy)-7,8-dihydro-5H-1,6-naphthyridin-6-yl]methanone 在 盐酸 作用下， 以 乙酸乙酯 为溶剂， 生成 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine
  参考文献：
  名称：

  An expeditious synthesis of 3-(difluoromethoxy)- and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines

  摘要：

  An expeditious and concise synthesis of 3-(difluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines is described. Starting from N-benzyl piperidone, the key intermediates leading to these two biologically desirable synthones were rapidly assembled by inverse electron demand Diels-Alder (IEDA) reaction utilizing microwave irradiation. The scope of the microwave methodology developed herein was extended to other ketones. (c) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2008.08.083

文献信息

• [EN] FUSED CYCLOPENTYL ANTAGONISTS OF CCR2<br/>[FR] ANTAGONISTES CYCLOPENTYLIQUES FUSIONNÉS DE CCR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2013152269A1

  公开（公告）日：2013-10-10

  The present invention comprises compounds of Formula (I). Formula (I) wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

  本发明涵盖了式（I）的化合物。式（I）中：R0、R1、R2、R3、R4、R5和A的定义如规范中所述。该发明还涵盖了一种预防、治疗或改善综合症、疾病或疾病的方法，其中所述综合症、疾病或疾病是2型糖尿病、肥胖和哮喘。该发明还涵盖了通过给哺乳动物施用至少一种式（I）化合物的治疗有效量来抑制CCR2活性的方法。
• FUSED CYCLOPENTYL ANTAGONISTS OF CCR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：US20150080588A1

  公开（公告）日：2015-03-19

  The present invention comprises processes for preparing compounds of Formula (I). wherein: R 0 , R 1 , R 2 , R 3 , R 4 , R 5 , and A are as defined in the specification.

  本发明涉及制备式（I）化合物的方法，其中：R0，R1，R2，R3，R4，R5和A如说明书所定义。
• US7230008B2
  申请人：——

  公开号：US7230008B2

  公开（公告）日：2007-06-12
• US7786305B2
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  公开（公告）日：2010-08-31
• US8822460B2
  申请人：——

  公开号：US8822460B2

  公开（公告）日：2014-09-02