7,8-bis(methyloxy)-10-[4-(methyloxy)phenyl]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indole | 869117-43-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: 7,8-bis(methyloxy)-10-[4-(methyloxy)phenyl]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indole
• 英文别名: 3,4-Dihydro-7,8-dimethoxy-10-(4-methoxyphenyl)-1H-[1,4]oxazino[4,3-a]indole；7,8-dimethoxy-10-(4-methoxyphenyl)-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indole
• CAS: 869117-43-1
• 化学式: C₂₀H₂₁NO₄
• 分子量: 339.391
• InChiKey: UCNZPMHYGWAUKW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  25
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  41.8
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  ethyl 5,6-dimethoxy-3-(4-methoxyphenyl)-1H-indole-2-carboxylate 在 lithium aluminium tetrahydride 、 potassium hydroxide 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 0.17h， 生成 7,8-bis(methyloxy)-10-[4-(methyloxy)phenyl]-3,4-dihydro-1H-[1,4]oxazino[4,3-a]indole
  参考文献：
  名称：

  Efficient and general synthesis of oxazino[4,3-a]indoles by cascade addition-cyclization reactions of (1H-indol-2-yl)methanols and vinyl sulfonium salts

  摘要：

  描述了一种高效且通用的氧杂氮并[4,3-a]吲哚结构的合成方法。将(1H-吲哚-2-基)醇与乙烯基磺盐的加成-环化级联反应可高产率获得氧杂氮并[4,3-a]吲哚衍生物。

  DOI：

  10.1039/c0cc03823g

文献信息

• Indole and Azaindole Derivatives with Antitumor Action
  申请人：Farina Carlo

  公开号：US20070248672A1

  公开（公告）日：2007-10-25

  Indole and azaindole compounds useful for the treatment of solid tumours and tumours of the blood are described, they being particularly effective in the treatment of drug resistant tumours; these compounds are also able to synergistically enhance the activity of known antitumour drugs. They can hence be used either alone as antitumour agents or in association with known antitumour drugs. Processes for preparing the aforesaid compounds, which are partly new, and pharmaceutical compositions useful for the aforesaid treatments are also described.

  本文描述了用于治疗实体肿瘤和血液肿瘤的吲哚和氮杂吲哚化合物，它们在治疗耐药性肿瘤方面特别有效；这些化合物还能够协同增强已知抗肿瘤药物的活性。因此，它们可以作为单独的抗肿瘤剂使用，也可以与已知的抗肿瘤药物联合使用。本文还描述了制备上述部分新化合物的过程以及用于上述治疗的制药组合物。
• V-ATPase inhibitors for the treatment of septic shock
  申请人：NIKEM RESEARCH S.R.L.

  公开号：EP1779849A1

  公开（公告）日：2007-05-02

  The use of vacuolar ATPase inhibitors in the prevention and/or treatment of septic shock is herein described. Vacuolar ATPase inhibitors are selected among products of natural, semi-synthetic or synthetic origin; more preferred are inhibitors based on a 2- and/or 3-substituted indole, azaindole or benzoimidazole structure.

  本文描述了空泡 ATP 酶抑制剂在预防和/或治疗脓毒性休克中的应用。空泡 ATP 酶抑制剂可从天然、半合成或合成产品中选择；更优选的是基于 2-和/或 3-取代的吲哚、氮杂环吲哚或苯并咪唑结构的抑制剂。
• V-ATPase inhibitors for the treatment of inflammatory and autoimmune diseases
  申请人：NIKEM RESEARCH S.R.L.

  公开号：EP1779848A1

  公开（公告）日：2007-05-02

  The use of vacuolar ATPase inhibitors in the prevention and/or treatment of inflammatory and autoimmune diseases is herein described. Vacuolar ATPase inhibitors are selected among products of natural, semi-synthetic or synthetic origin; more preferred are inhibitors based on a 2- and/or 3-substituted indole, azaindole or benzimidazole structure.

  本文描述了空泡 ATP 酶抑制剂在预防和/或治疗炎症和自身免疫性疾病中的应用。空泡 ATP 酶抑制剂可从天然、半合成或合成产品中选择；更优选的是基于 2-和/或 3-取代的吲哚、氮杂环吲哚或苯并咪唑结构的抑制剂。
• INDOLE AND AZAINDOLE DERIVATIVES WITH ANTITUMOR ACTION
  申请人：NIKEM RESEARCH S.R.L.

  公开号：EP1750687A2

  公开（公告）日：2007-02-14
• Indole and Azaindole Derivatives For the Treatment of Inflammatory and Autoimmune Diseases
  申请人：Farina Carlo

  公开号：US20080226718A1

  公开（公告）日：2008-09-18

  The use is described of compounds of formula (I) wherein A is chosen from a phenyl or a heterocyclic ring with 5 or 6 members containing up to two heteroatoms chosen from nitrogen, oxygen and sulfur, X and Y represent carbon or nitrogen, and R1-R6 are as described in the specification, in the prevention and/or treatment of inflammatory and autoimmune diseases.