2,6-Ditert-butyl-4-[[(6-methoxypyridin-3-yl)amino]methyl]phenol | 357614-87-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2,6-Ditert-butyl-4-[[(6-methoxypyridin-3-yl)amino]methyl]phenol
• 英文别名: 2,6-ditert-butyl-4-[[(6-methoxypyridin-3-yl)amino]methyl]phenol
• CAS: 357614-87-0
• 化学式: C₂₁H₃₀N₂O₂
• 分子量: 342.481
• InChiKey: MGIUTCHYHRSLFP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  54.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,6-Ditert-butyl-4-[[(6-methoxypyridin-3-yl)amino]methyl]phenol 、 对甲苯磺酰氯 在 吡啶 、 4-二甲氨基吡啶 作用下， 反应 18.0h， 生成 N-(3,5-di-tert-butyl-4-hydroxybenzyl)-N-(6-methoxypyridin-3-yl)-4-methylbenzenesulfonamide
  参考文献：
  名称：

  Inhibitors of lipoprotein(a) assembly

  摘要：

  Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral closing of compound 14-6 to Lp(a) transgenic mice and cymologous monkeys resulted in a > 30% decrease in plasma Lp(a) levels after 1-2 weeks of treatment at 100 mg/kg/day.) (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2002.04.001
• 作为产物：
  描述：

  3,5-二叔丁基-4-羟基苯甲醛 在 RaNi 氢气 、 对甲苯磺酸 作用下， 以 四氢呋喃 、 甲醇 、 甲苯 为溶剂， 生成 2,6-Ditert-butyl-4-[[(6-methoxypyridin-3-yl)amino]methyl]phenol
  参考文献：
  名称：

  Inhibitors of lipoprotein(a) assembly

  摘要：

  Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral closing of compound 14-6 to Lp(a) transgenic mice and cymologous monkeys resulted in a > 30% decrease in plasma Lp(a) levels after 1-2 weeks of treatment at 100 mg/kg/day.) (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2002.04.001

文献信息

• Sulfonamide compounds and methods of treating atherosclerosis and restenosis
  申请人：——

  公开号：US20010018523A1

  公开（公告）日：2001-08-30

  The present invention provides compounds having the Formula I 1 The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

  本发明提供具有化学式I的化合物。本发明还提供利用化合物I治疗或预防动脉粥样硬化、冠心病和再狭窄的方法，以及包含化合物I的药物组合物。
• US6284795B1
  申请人：——

  公开号：US6284795B1

  公开（公告）日：2001-09-04
• US6458815B2
  申请人：——

  公开号：US6458815B2

  公开（公告）日：2002-10-01
• Inhibitors of lipoprotein(a) assembly
  作者：Karen E Sexton、Helen T Lee、Mark Massa、Janak Padia、William C Patt、Peggy Liao、Jason K Pontrello、Bruce D Roth、Mark A Spahr、Randy Ramharack

  DOI：10.1016/j.bmc.2002.04.001

  日期：2003.11

  Compounds of the general structure A and B were investigated for their activity as lipoprotein(a), [Lp(a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral closing of compound 14-6 to Lp(a) transgenic mice and cymologous monkeys resulted in a > 30% decrease in plasma Lp(a) levels after 1-2 weeks of treatment at 100 mg/kg/day.) (C) 2003 Elsevier Ltd. All rights reserved.