N-(4,5-dihydronaphtho[1,2-d][1,3]thiazol-2-yl)propanamide | 391229-55-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 萘并噻唑类
• 英文名称: N-(4,5-dihydronaphtho[1,2-d][1,3]thiazol-2-yl)propanamide
• 英文别名: N-(4,5-dihydrobenzo[e][1,3]benzothiazol-2-yl)propanamide
• CAS: 391229-55-3
• 化学式: C₁₄H₁₄N₂OS
• 分子量: 258.344
• InChiKey: KPTBRESUDPEAAU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  70.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-(4,5-dihydronaphtho[1,2-d][1,3]thiazol-2-yl)propanamide 在 lithium aluminium tetrahydride 、 sodium sulfate 作用下， 以 四氢呋喃 为溶剂， 反应 4.0h， 以82%的产率得到N-propyl-4,5-dihydronaphtho[1,2-d][1,3]thiazol-2-amine
  参考文献：
  名称：

  RECEPTOR FUNCTION CONTROLLING AGENT

  摘要：

  公开号：

  EP1559422B1
• 作为产物：
  描述：

  4,5-二氢萘并[1,2-d]噻唑-2-胺 、 丙酰氯 在 吡啶 作用下， 反应 2.0h， 以91%的产率得到N-(4,5-dihydronaphtho[1,2-d][1,3]thiazol-2-yl)propanamide
  参考文献：
  名称：

  RECEPTOR FUNCTION CONTROLLING AGENT

  摘要：

  公开号：

  EP1559422B1

文献信息

• Receptor Function Regulator
  申请人：Fukatsu Kohji

  公开号：US20090012093A1

  公开（公告）日：2009-01-08

  The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

  本发明的GPR40受体功能调节剂包括具有芳香环和能够释放阳离子的基团的化合物，可用作胰岛素分泌剂或预防或治疗糖尿病等疾病的药剂。
• Receptor function regulator
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US07960369B2

  公开（公告）日：2011-06-14

  The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

  本发明的GPR40受体功能调节剂，包括具有芳香环和能够释放阳离子的基团的化合物，可用作胰岛素促分泌剂或预防或治疗糖尿病等药物。
• GPR40 Receptor function regulator
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2385032A1

  公开（公告）日：2011-11-09

  The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

  本发明的 GPR40 受体功能调节剂由具有芳香环和能够释放阳离子的基团的化合物组成，可用作胰岛素分泌剂或预防或治疗糖尿病等的药物。
• Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers
  作者：Anikó Göblyös、Sabrina Neves Santiago、Daniele Pietra、Thea Mulder-Krieger、Jacobien von Frijtag Drabbe Künzel、Johannes Brussee、Adriaan P. IJzerman

  DOI：10.1016/j.bmc.2005.01.006

  日期：2005.3

  A number of 2-aminothiazoles (2a-e) and their amide derivatives (4-10) were prepared. The 2-aminothiazoles themselves were tested as allosteric enhancers of agonist binding to human adenosine A, receptors. In a variety of experimental set-ups the compounds did not show any such effect, in contrast to earlier findings by another research group. Subsequently the 2-aminothiazoles were used as intermediates in the synthesis of a number of amide derivatives of either aromatic (4-6) or aliphatic nature (7-10). Some of the compounds emerged as moderately active antagonists on human adenosine A(1) and/or A(2A) receptors with lower or negligible potency at adenosine A(3) receptors. (c) 2005 Elsevier Ltd. All rights reserved.
• US7960369B2
  申请人：——

  公开号：US7960369B2

  公开（公告）日：2011-06-14