2-amino-5-(4-methyl-1-piperazinyl)-Phenol | 126824-10-0

• 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: 2-amino-5-(4-methyl-1-piperazinyl)-Phenol
• 英文别名: 2-amino-5-(4-methylpiperazin-1-yl)phenol
• CAS: 126824-10-0
• 化学式: C₁₁H₁₇N₃O
• 分子量: 207.275
• InChiKey: CUNQCKLRNYHINB-UHFFFAOYSA-N

物化性质

• 沸点：
  399.7±42.0 °C(Predicted)
• 密度：
  1.194±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  52.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8-indan-5-yl-2-methanesulfonyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester 、 2-amino-5-(4-methyl-1-piperazinyl)-Phenol 以 异丙醇 为溶剂， 生成
  参考文献：
  名称：

  Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors

  摘要：

  A series of pyrimidinopyridones has been designed, synthesized and shown to be potent and selective inhibitors of the FMS tyrosine kinase. Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase. Compound 24 effectively inhibited in vivo LPS-induced TNF in mice greater than 80%. (C) 2008 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2008.02.070
• 作为产物：
  描述：

  5-氟-2-硝基苯酚 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 、 乙腈 为溶剂， 反应 5.0h， 生成 2-amino-5-(4-methyl-1-piperazinyl)-Phenol
  参考文献：
  名称：

  2-Aminobenzoxazole ligands of the hepatitis C virus internal ribosome entry site

  摘要：

  2-Aminobenzoxazoles have been synthesized as ligands for the hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA. The compounds were designed to explore the less basic benzoxazole system as a replacement for the core scaffold in previously discovered benzimidazole viral translation inhibitors. Structure-activity relationships in the target binding of substituted benzoxazole ligands were investigated. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.05.088

文献信息

• 5-Oxo-5,8-dihydro-pyrido-pyrimidines as inhibitors of c-fms kinase
  申请人：Player R. Mark

  公开号：US20070060577A1

  公开（公告）日：2007-03-15

  The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R 101 and R 200 are described in the specification.

  该发明通过提供c-fms激酶的有效抑制剂来解决当前对选择性和强效蛋白酪氨酸激酶抑制剂的需求。该发明涉及公式I的新化合物：或其溶剂化合物、水合物、互变异构体或药用可接受的盐，其中：W、A、Y、Z、R101和R200如规范中所述。
• 5-oxo-5,8-dihydro-pyrido-pyrimidine as inhibitors of c-fms kinase
  申请人：Janssen Pharmaceutica N.V.

  公开号：US07642270B2

  公开（公告）日：2010-01-05

  The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R101 and R200 are described in the specification.

  本发明旨在提供c-fms激酶的有效抑制剂，以满足当前选择性和强效蛋白酪氨酸激酶抑制剂的需求。本发明涉及公式I的新型化合物：或其溶剂化物、水合物、互变异构体或药学上可接受的盐，其中：W、A、Y、Z、R101和R200在说明书中描述。
• 5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE
  申请人：Janssen Pharmaceutica NV

  公开号：EP1937681A1

  公开（公告）日：2008-07-02
• US7642270B2
  申请人：——

  公开号：US7642270B2

  公开（公告）日：2010-01-05
• [EN] 5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE<br/>[FR] 5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES COMME INHIBITEURS DE KINASE C-FMS
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2007033232A1

  公开（公告）日：2007-03-22

  [EN] The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula (I) or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof, wherein: W, A, Y, Z, R¹⁰¹ and R²⁰⁰ are described in the specification.
  [FR] L'invention concerne le besoin actuel d'inhibiteurs sélectifs et puissants de la protéine tyrosine kinase qui consiste à fournir des inhibiteurs puissants de kinase C-FMS. L'invention concerne les nouveaux composés de la formule I; ou un solvate, un hydrate, un tautomère ou un sel pharmaceutiquement acceptable de ceux-ci. W, A, Y, Z, R¹⁰¹ et R²⁰⁰ sont précisés dans le descriptif.