1-[5-methyl-6-(2-methyl-5-trifluoromethyl-2H-pyrazol-3-yloxy)-pyrimidin-4-yl]-piperidine-4-carboxylic acid ethyl ester | 733748-24-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[5-methyl-6-(2-methyl-5-trifluoromethyl-2H-pyrazol-3-yloxy)-pyrimidin-4-yl]-piperidine-4-carboxylic acid ethyl ester
• 英文别名: Ethyl 1-[5-methyl-6-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]oxypyrimidin-4-yl]piperidine-4-carboxylate
• CAS: 733748-24-8
• 化学式: C₁₈H₂₂F₃N₅O₃
• 分子量: 413.4
• InChiKey: LJBUXCRZSXVPKW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  29
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  82.4
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  1-[5-bromo-6-(2-methyl-5-trifluoromethyl-2H-pyrazol-3-yloxy)-pyrimidin-4-yl]-piperidine-4-carboxylic acid ethyl ester 、 甲基硼酸 在 bis-triphenylphosphine-palladium(II) chloride potassium carbonate 作用下， 以 DMF (N,N-dimethyl-formamide) 为溶剂， 以23%的产率得到1-[5-methyl-6-(2-methyl-5-trifluoromethyl-2H-pyrazol-3-yloxy)-pyrimidin-4-yl]-piperidine-4-carboxylic acid ethyl ester
  参考文献：
  名称：

  [EN] 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PRPPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO SUCH AS DIABETES AND HYPERGLYCEMIA
  [FR] DERIVES ARYLES ET HETEROARYLES TRI-SUBSTITUES EN POSITION 1,2,3 EN TANT QUE MODULATEURS DE METABOLISME ET PROPHYLAXIE ET TRAITEMENT DE TROUBLES LIES AU METABOLISME

  摘要：

  本发明涉及某些Fomula（Ia）的1,2,3-三取代芳基和杂芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢紊乱及其并发症，如糖尿病和肥胖方面是有用的。

  公开号：

  WO2004065380A1

文献信息

• 1,2,3-Trisubstituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto such as diabetes and hyperglycemia
  申请人：Jones M. Robert

  公开号：US20060217379A1

  公开（公告）日：2006-09-28

  The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及某些1,2,3-三取代芳基和杂环芳基衍生物（Ia式）的代谢调节剂。因此，本发明的化合物在预防或治疗代谢性疾病及其并发症，如糖尿病和肥胖症方面是有用的。
• 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO SUCH AS DIABETES AND HYPERGLYCEMIA
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1599468B1

  公开（公告）日：2007-10-03
• US8293751B2
  申请人：——

  公开号：US8293751B2

  公开（公告）日：2012-10-23
• US8933083B2
  申请人：——

  公开号：US8933083B2

  公开（公告）日：2015-01-13
• [EN] 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PRPPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO SUCH AS DIABETES AND HYPERGLYCEMIA<br/>[FR] DERIVES ARYLES ET HETEROARYLES TRI-SUBSTITUES EN POSITION 1,2,3 EN TANT QUE MODULATEURS DE METABOLISME ET PROPHYLAXIE ET TRAITEMENT DE TROUBLES LIES AU METABOLISME
  申请人：ARENA PHARM INC

  公开号：WO2004065380A1

  公开（公告）日：2004-08-05

  The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.

  本发明涉及某些Fomula（Ia）的1,2,3-三取代芳基和杂芳基衍生物，它们是代谢调节剂。因此，本发明的化合物在预防或治疗代谢紊乱及其并发症，如糖尿病和肥胖方面是有用的。