4-amino-5-(naphth-2-oyl)-2-phenylaminothiazole

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 4-amino-5-(naphth-2-oyl)-2-phenylaminothiazole
• 英文别名: (4-amino-2-phenylaminothiazol-5-yl)naphthalen-2-ylmethanone；(4-Amino-2-anilino-1,3-thiazol-5-yl)-naphthalen-2-ylmethanone；(4-amino-2-anilino-1,3-thiazol-5-yl)-naphthalen-2-ylmethanone
• 化学式: C₂₀H₁₅N₃OS
• 分子量: 345.425
• InChiKey: RKBALHPGBQMZOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  96.2
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  硫代异氰酸苯酯 在 三乙胺 、 sodium hydroxide 作用下， 以 二甲基亚砜 为溶剂， 反应 1.0h， 生成 4-amino-5-(naphth-2-oyl)-2-phenylaminothiazole
  参考文献：
  名称：

  One-pot sequential multicomponent route to 2,4-diaminothiazoles—a facile approach to bioactive agents for cancer therapeutics

  摘要：

  A facile one-pot sequential three-component route to 2,4-diaminothiazoles is reported. The new approach employs the mildest reaction conditions and commercially available reagents to generate diverse 2-alkyl/arylamino-4-amino-5-aroyl/heteroylthiazoles in short reaction times, good yield, and purity. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2012.05.010

文献信息

• Inhibitors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma
  申请人：——

  公开号：US20040186159A1

  公开（公告）日：2004-09-23

  The use of inhibitors of GSK-3 useful for treating glaucoma is disclosed.

  抑制GSK-3用于治疗青光眼的方法被揭示。
• Use of 2,4-diaminothiazole derivatives
  申请人：——

  公开号：US20010039275A1

  公开（公告）日：2001-11-08

  2,4-Diaminothiazole derivatives which inhibit GSK-3 (glycogen synthase kinase-3) and which are useful for the treatment and/or prevention disorders and diseases wherein an inhibition of GSK-3 is beneficial, especially especially Alzheimer's disease, bipolar disorder, IGT (impaired glucose tolerance), Type 1 diabetes, Type 2 diabetes and obesity.

  抑制GSK-3（糖原合成激酶-3）的2,4-二氨基噻唑衍生物，对治疗和/或预防GSK-3抑制有益的疾病和疾病特别有效，尤其是阿尔茨海默病、双相情感障碍、糖耐量受损（IGT）、1型糖尿病、2型糖尿病和肥胖症。
• An efficient protocol for solid phase aminothiazole synthesis
  作者：Kumaran G. Sreejalekshmi、Satyabhama K.C. Devi、Kallikat N. Rajasekharan

  DOI：10.1016/j.tetlet.2006.06.169

  日期：2006.8

  An efficient synthesis of 2,4-diamino-5-ketothiazoles under solid phase conditions has been achieved by the reaction of polymer supported amidinothioureas with α-haloketones. This novel synthetic approach involving traceless cleavage from the support is suited for automation, and allows solid phase combinatorial synthesis of 2,4-diamino-5-ketothiazoles in good yields and purities.

  在固相条件下，通过聚合物负载的mid基硫脲与α-卤代酮的反应已实现了2,4-二氨基-5-酮噻唑的有效合成。这种涉及从载体上无痕裂解的新颖合成方法适用于自动化，并允许以良好的收率和纯度进行固相组合合成2,4-二氨基-5-酮噻唑。
• [EN] 2,4-DIAMINOTHIAZOLE DERIVATIVES AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 (GSK-3) INHIBITORS<br/>[FR] DERIVES DE 2,4-DIAMINOTHIAZOLE
  申请人：NOVO NORDISK AS

  公开号：WO2001056567A1

  公开（公告）日：2001-08-09

  2,4-Diaminothiazole derivatives which inhibit GSK-3 (glycogen synthase kinase-3) and which are useful for the treatment and/or prevention disorders and diseases wherein an inhibition of GSK-3 is beneficial, especially especially Alzheimer's disease, bipolar disorder, IGT (impaired glucose tolerance), Type 1 diabetes, Type 2 diabetes and obesity.

  2,4-二氨基噻唑衍生物抑制GSK-3（糖原合成酶激酶-3），对于治疗和/或预防抑制GSK-3有益的疾病和疾病特别是阿尔茨海默病、双相情感障碍、IGT（糖耐量受损）、1型糖尿病、2型糖尿病和肥胖症具有用处。
• Inhibitors of glycogen synthase kinase-3 (GSK-3) for treating glaucomatous optic neuropathy
  申请人：Alcon, Inc.

  公开号：EP2281560A1

  公开（公告）日：2011-02-09

  The use of inhibitors of GSK-3 useful for treating, preventing or inhibiting glaucoma, including treating glaucomatous optic neuropathy, is disclosed.

  本研究公开了用于治疗、预防或抑制青光眼（包括治疗青光眼性视神经病变）的 GSK-3 抑制剂的用途。