2-chloro-4-cyclobutoxy-5-fluoro-pyrimidine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-chloro-4-cyclobutoxy-5-fluoro-pyrimidine
• 英文别名: 2-Chloro-4-cyclobutoxy-5-fluoropyrimidine；2-chloro-4-cyclobutyloxy-5-fluoropyrimidine
• 化学式: C₈H₈ClFN₂O
• 分子量: 202.616
• InChiKey: APUYEPKEAQVHKI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  环丁醇 、 2,4-二氯-5-氟嘧啶 以 四氢呋喃 、 mineral oil 为溶剂， 反应 16.17h， 生成 2-chloro-4-cyclobutoxy-5-fluoro-pyrimidine
  参考文献：
  名称：

  [EN] TETRAHYDRO-BENZO[D]AZEPINE DERIVATIVES AS GPR120 MODULATORS
  [FR] DÉRIVÉS DE TÉTRAHYDRO-BENZO[D]AZÉPINE UTILISÉS EN TANT QUE MODULATEURS DE GPR120

  摘要：

  具有以下式（I）的新型四氢异喹啉和四氢苯并哌啶化合物能够调节G蛋白偶联受体GPR120，包括这些化合物的组合物，以及用于调控体内胰岛素水平和治疗糖尿病、炎症、肥胖和代谢性疾病等症状的方法。

  公开号：

  WO2018172727A1

文献信息

• BIARYL DERIVATIVE AS GPR120 AGONIST
  申请人：LG Chem, Ltd.

  公开号：EP3239143A2

  公开（公告）日：2017-11-01

  The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

  本发明涉及一种由化学式1表示的生物芳基衍生物、生产该生物芳基衍生物的方法、包含该生物芳基衍生物的药物组合物以及该生物芳基衍生物的用途，由化学式1表示的生物芳基衍生物作为GPR120激动剂，促进胃肠道中GLP-1的生成、从巨噬细胞、胰腺细胞等的抗炎活性中降低肝脏、肌肉等的胰岛素抵抗，并可有效用于预防或治疗炎症或代谢性疾病，如糖尿病、糖尿病并发症、肥胖症、非酒精性脂肪肝、脂肪肝和骨质疏松症。
• Tetrahydro-benzo[d]azepine derivatives as GPR120 modulators
  申请人：CALDAN THERAPEUTICS LIMITED

  公开号：US11220483B2

  公开（公告）日：2022-01-11

  Novel tetrahydroisoquinoline and tetrahydrobenzazepine compounds of formula (I) capable of modulating the G-protein-coupled receptor GPR120, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as of diabetes, inflammation, obesity and metabolic diseases.

  能够调节 G 蛋白偶联受体 GPR120 的新型式 (I) 四氢异喹啉和四氢苯并氮杂卓化合物、包含这些化合物的组合物，以及将其用于控制体内胰岛素水平和治疗糖尿病、炎症、肥胖症和代谢性疾病等病症的方法。
• Biaryl derivative as GPR120 agonist
  申请人：LG CHEM, LTD.

  公开号：US11261186B2

  公开（公告）日：2022-03-01

  Compounds having the chemical formula 1, a method for producing the compounds of chemical formula 1, a pharmaceutical composition comprising same, and use thereof as a GPR120 agonist for prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.

  具有化学式1的化合物，制备所述化学式1化合物的方法，包含所述化合物的药物组合物，以及将其用作一种GPR120激动剂，用于预防或治疗炎症或代谢性疾病，如糖尿病、糖尿病并发症、肥胖症、非酒精性脂肪肝病、脂肪肝病和骨质疏松症。
• TETRAHYDRO-BENZO[D]AZEPINE DERIVATIVES AS GPR120 MODULATORS
  申请人：CALDAN THERAPEUTICS LIMITED

  公开号：US20200317619A1

  公开（公告）日：2020-10-08

  Novel tetrahydroisoquinoline and tetrahydrobenzazepine compounds of formula (I) capable of modulating the G-protein-coupled receptor GPR120, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as of diabetes, inflammation, obesity and metabolic diseases. (I)
• [EN] TETRAHYDRO-BENZO[D]AZEPINE DERIVATIVES AS GPR120 MODULATORS<br/>[FR] DÉRIVÉS DE TÉTRAHYDRO-BENZO[D]AZÉPINE UTILISÉS EN TANT QUE MODULATEURS DE GPR120
  申请人：CALDAN THERAPEUTICS LTD

  公开号：WO2018172727A1

  公开（公告）日：2018-09-27

  Novel tetrahydroisoquinoline and tetrahydrobenzazepine compounds of formula (I) capable of modulating the G-protein-coupled receptor GPR120, compositions comprising the compounds, and methods for their use for controlling insulin levelsin vivoand for the treatment of conditions such as of diabetes, inflammation, obesity and metabolic diseases. (I)

  具有以下式（I）的新型四氢异喹啉和四氢苯并哌啶化合物能够调节G蛋白偶联受体GPR120，包括这些化合物的组合物，以及用于调控体内胰岛素水平和治疗糖尿病、炎症、肥胖和代谢性疾病等症状的方法。