6-nitro-2-piperazin-1-yl-benzothiazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 6-nitro-2-piperazin-1-yl-benzothiazole
• 英文别名: 6-nitro-2-(piperazin-1-yl)benzothiazole；6-Nitro-2-piperazin-1-yl-1,3-benzothiazole
• 化学式: C₁₁H₁₂N₄O₂S
• 分子量: 264.308
• InChiKey: RBZWYLUVTPLLOU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  102
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-nitro-2-piperazin-1-yl-benzothiazole 在 palladium 10% on activated carbon 氢气 作用下， 以 四氢呋喃 为溶剂， 反应 19.0h， 以60%的产率得到6-amino-2-(piperazin-1-yl)benzothiazole
  参考文献：
  名称：

  WO2008/153325

  摘要：

  公开号：
• 作为产物：
  描述：

  哌嗪 、 2-氯-6-硝基苯并噻唑 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 0.17h， 生成 6-nitro-2-piperazin-1-yl-benzothiazole
  参考文献：
  名称：

  Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups

  摘要：

  本发明涉及一般式I的化合物，其中R1是该基团，而R2、R′、R″、R3、R4、R5、R6、R7、X1、X1′、X2和N如规范中所定义。本发明的化合物对治疗神经和神经精神疾病有用。

  公开号：

  US20060128712A1

文献信息

• Chemospecific and ligand free CuI catalysed heterogeneous N-arylation of amines with diheteroaryl halides at room temperature
  作者：Sanjeev K. Verma、B. N. Acharya、M. P. Kaushik

  DOI：10.1039/c0ob00859a

  日期：——

  A ligand free, copper-catalyzed N-arylation reaction of amines with diheteroaryl halides in heterogeneous medium at room temperature has been developed. The protocol is very effective for low boiling amines and useful for amines available in aqueous solution. The reaction gives chemospecific arylation of amines with diheteroaryl halides in the mixture monoheteroaryl halides, diheteroaryl halides and carbocyclic aryl halides. The reaction is also chemospecific with respect to arylation of aliphatic amines. Monoarylated piperazines were also synthesized at room temperature following this protocol.

  我们开发了一种无配体、铜催化的 N-芳基化反应，可在室温下在异相介质中使胺与二硬脂酰卤发生反应。该方案对低沸点胺非常有效，对水溶液中的胺也很有用。在单杂芳基卤化物、二杂芳基卤化物和碳环芳基卤化物的混合物中，该反应可使胺与二杂芳基卤化物发生化学特异性芳基化反应。该反应对脂肪胺的芳基化也具有化学特异性。按照此方案，还可在室温下合成单芳基化的哌嗪。
• Proline derivatives and use thereof as drugs
  申请人：Kitajima Hiroshi

  公开号：US20050245538A1

  公开（公告）日：2005-11-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗效果的化合物，其作用是通过DPP-IV的抑制作用，并且作为药物产品具有令人满意的效果。本发明人发现，在丙氨酸的γ位上引入取代基的衍生物具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。
• Proline derivatives and the use thereof as drugs
  申请人：——

  公开号：US20040106655A1

  公开（公告）日：2004-06-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the &ggr;-position of proline represented by the formula (I) 1 wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗作用的化合物，由于DPP-IV抑制作用而具有满意的药物产品。本发明人发现，具有引入取代基的脯氨酸γ-位置的衍生物，其化学式为(I)1，其中每个符号如规范中所定义，具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。
• TRIAZOLE DERIVATIVES HAVING ANTIFUNGAL ACTIVITY, METHOD FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：Kim Bum Tae

  公开号：US20100144712A1

  公开（公告）日：2010-06-10

  A triazole derivative of formula 1 or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof is superior to the conventional antifungal drugs in antifungal activity against a wide spectrum of pathogenic fungi, and has advantageously low toxicity.

  1号公式的三唑衍生物或其药学上可接受的盐、水合物、溶剂合物或异构体，在抗击广谱病原真菌的抗真菌活性方面优于传统的抗真菌药物，并具有低毒性的优势。
• PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1308439B1

  公开（公告）日：2008-10-15