1-iodo-5-phthalimidohexane | 82082-24-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 1-iodo-5-phthalimidohexane
• 英文别名: 2-(6-iodohexan-2-yl)isoindole-1,3-dione
• CAS: 82082-24-4
• 化学式: C₁₄H₁₆INO₂
• 分子量: 357.191
• InChiKey: DNTFZLZXHSSXBD-UHFFFAOYSA-N

物化性质

• 熔点：
  48-50 °C(Solv: ligroine (8032-32-4))
• 沸点：
  407.1±28.0 °C(Predicted)
• 密度：
  1.601±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.28
• 重原子数：
  18.0
• 可旋转键数：
  5.0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  37.38
• 氢给体数：
  0.0
• 氢受体数：
  2.0

反应信息

• 作为反应物：
  描述：

  1-iodo-5-phthalimidohexane 在 一水合肼 、 三乙胺 作用下， 以 乙二醇乙醚 、 乙醇 为溶剂， 反应 3.0h， 生成 N¹-(5,6-Dimethoxy-4-methyl-quinolin-8-yl)-hexane-1,5-diamine
  参考文献：
  名称：

  Antimalarials. 13. 5-Alkoxy analogs of 4-methylprimaquine

  摘要：

  A series of nuclear and side-chain analogues of 4-methylprimaquine incorporating an alkoxy group in the 5-position of the quinoline nucleus has been prepared. The compounds were tested for suppressive antimalarial activity against Plasmodium berghei in mice and for radical curative antimalarial activity against Plasmodium cynomolgi in the rhesus monkey. Although the toxicity problems characteristic of the 8-aminoquinolines were not overcome, several of the compounds, surprisingly, were highly effective as both blood and tissue schizonticidal agents.

  DOI：

  10.1021/jm00350a016
• 作为产物：
  描述：

  5,6-二氢-3-乙氧羰基-2-甲基-4H-吡喃 在 镍 盐酸 、 ammonium hydroxide 、 氯化亚砜 、 氢气 、 sodium iodide 作用下， 以 丙酮 、 xylene 、 苯 为溶剂， 反应 40.0h， 生成 1-iodo-5-phthalimidohexane
  参考文献：
  名称：

  Antimalarials. 13. 5-Alkoxy analogs of 4-methylprimaquine

  摘要：

  A series of nuclear and side-chain analogues of 4-methylprimaquine incorporating an alkoxy group in the 5-position of the quinoline nucleus has been prepared. The compounds were tested for suppressive antimalarial activity against Plasmodium berghei in mice and for radical curative antimalarial activity against Plasmodium cynomolgi in the rhesus monkey. Although the toxicity problems characteristic of the 8-aminoquinolines were not overcome, several of the compounds, surprisingly, were highly effective as both blood and tissue schizonticidal agents.

  DOI：

  10.1021/jm00350a016

文献信息

• Antimalarials. 15. Side-chain analogues of 8-(4-amino-1-methylbutylamino)-6-methoxy-4-methyl-5-(3-trifluoromethylphenoxy)quinoline
  作者：Maurice P. Lamontagne、Peter Blumbergs

  DOI：10.1002/jhet.5570210108

  日期：1984.1

  Six side chain analogs of the highly active antimalarial agent 8-(4-amino-1-methylbutylamino)-6-methoxy-4-methyl-5-(3-trifluoromethylphenoxy)quinoline (I) were prepared and evaluated for blood and tissue schizonticidal activity. Although most examples were markedly superior to primaquine none was superior to the parent compound I.

  制备了六种高活性抗疟疾药物8-（4-氨基-1-甲基丁基氨基）-6-甲氧基-4-甲基-5-（3-三氟甲基苯氧基）喹啉（I）的侧链类似物，并对其血液和组织裂殖体进行了评估活动。尽管大多数实例均明显优于伯氨喹，但均未优于母体化合物I。
• LAMONTAGNE, M. P.;MARKOVAC, A.;KHAN, M. S., J. MED. CHEM., 1982, 25, N 3, 964-968
  作者：LAMONTAGNE, M. P.、MARKOVAC, A.、KHAN, M. S.

  DOI：——

  日期：——
• LAMONTAGNE, M. P.;BLUMBERGS, P., J. HETEROCYCL. CHEM., 1984, 21, N 1, 33-35
  作者：LAMONTAGNE, M. P.、BLUMBERGS, P.

  DOI：——

  日期：——