6-Dimethoxymethyl-pyrimidin-4-ol | 500695-15-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-Dimethoxymethyl-pyrimidin-4-ol
• 英文别名: 4-(dimethoxymethyl)-1H-pyrimidin-6-one
• CAS: 500695-15-8
• 化学式: C₇H₁₀N₂O₃
• mdl: MFCD11106709
• 分子量: 170.168
• InChiKey: CDKZTTXJWHFHAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.1
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.428
• 拓扑面积：
  59.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-Dimethoxymethyl-pyrimidin-4-ol 在 三氯氧磷 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  Pyrimidinylimidazole inhibitors of CSBP/P38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes

  摘要：

  Pyrimidine analogs of the pyridinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinyl compounds. The substitution of pyrimidin-4-yl, 2-methoxypyrimidin-4-yl, or 2-methylaminopyrimidin-4-yl for pyridin-4-yl effectively dissociates CSBP/p38 kinctse from P450 inhibition for this series and furthermore achieves an increase in oral activity. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00549-6
• 作为产物：
  描述：

  ethyl 4,4-dimethoxy-3-oxobutanoate 、 醋酸甲脒 在 氢氧化钾 作用下， 以 乙醇 为溶剂， 生成 6-Dimethoxymethyl-pyrimidin-4-ol
  参考文献：
  名称：

  Pyrimidinylimidazole inhibitors of CSBP/P38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes

  摘要：

  Pyrimidine analogs of the pyridinylimidazole class of CSBP/p38 kinase inhibitors were prepared in an effort to reduce the potent inhibition of hepatic cytochrome P450 observed for the pyridinyl compounds. The substitution of pyrimidin-4-yl, 2-methoxypyrimidin-4-yl, or 2-methylaminopyrimidin-4-yl for pyridin-4-yl effectively dissociates CSBP/p38 kinctse from P450 inhibition for this series and furthermore achieves an increase in oral activity. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(98)00549-6

文献信息

• Substituted alkylamine derivatives and methods of use
  申请人：Amgen Inc.

  公开号：US20030225106A1

  公开（公告）日：2003-12-04

  Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的胺对预防治疗疾病有效，如血管生成介导的疾病。本发明包括新的化合物、类似物、前药和药用可接受的盐，药物组合物和预防治疗疾病和其他疾病或状况的方法，包括癌症等。本发明还涉及制造这类化合物的过程以及在此类过程中有用的中间体。
• [EN] SUBSTITUTED 2-ALKYLAMINE NICOTINIC AMIDE DERIVATIVES AND USE THERE OF<br/>[FR] DERIVES SUBSTITUES D'AMIDE 2-ALKYLAMINE NICOTINIQUE ET UTILISATIONS ASSOCIEES
  申请人：AMGEN INC

  公开号：WO2004007458A1

  公开（公告）日：2004-01-22

  Selected amines of Formula XIII, which are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的十三号化合物，对于预防和治疗疾病，如介导血管生成的疾病具有有效性。该发明包括新的化合物、类似物、前药和药学上可接受的盐，药物组合物以及用于预防和治疗癌症等疾病和其他病症或状况的方法。该发明还涉及制造这些化合物的过程以及在这些过程中有用的中间体。
• Process for preparing 3,3-dimethylindolines
  申请人：Amgen Inc.

  公开号：US07687643B2

  公开（公告）日：2010-03-30

  Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的胺类物质对于预防和治疗疾病，如血管生成介导的疾病具有有效作用。该发明涵盖了新型化合物、类似物、前药和其药学上可接受的盐、制药组合物和用于预防和治疗涉及癌症等疾病和其他疾病或病症的方法。该发明还涉及制备这些化合物的过程以及在这些过程中有用的中间体。
• SUBSTITUTED 2-ALKYLAMINE NICOTINIC AMIDE DERIVATIVES AND USE THERE OF
  申请人：AMGEN INC.

  公开号：EP1537084B1

  公开（公告）日：2013-08-21
• US6878714B2
  申请人：——

  公开号：US6878714B2

  公开（公告）日：2005-04-12