3-(Indol-3-yl)-8-azabicyclo[3.2.1]octane

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 3-(Indol-3-yl)-8-azabicyclo[3.2.1]octane
• 英文别名: 3-(8-azabicyclo[3.2.1]octan-3-yl)-1H-indole
• 化学式: C₁₅H₁₈N₂
• 分子量: 226.32
• InChiKey: OMUWOOCASHIXLS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  27.8
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  3-(8-aza-bicyclo[3.2.1]oct-2-en-3-yl)-1H-indole 在 钯 作用下， 以to give the corresponding 3-(indol-3-yl)-8-azabicyclo[3.2.1]octane的产率得到3-(Indol-3-yl)-8-azabicyclo[3.2.1]octane
  参考文献：
  名称：

  Inhibition of serotonin reuptake

  摘要：

  本发明提供了对哺乳动物中的血清素再摄取有用的3-（双环杂环芳基）-8-氮杂双环[3.2.1]辛-2-烯和3-（双环杂环芳基）-8-氮杂双环[3.2.1]辛烷。

  公开号：

  US06107307A1

文献信息

• Azabicyclic inhibitors of serotonin reuptake
  申请人：ELI LILLY AND COMPANY

  公开号：EP0969005A1

  公开（公告）日：2000-01-05

  This invention provides 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]oct-2-enes and 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]octanes of furmula (I) which are useful for the inhibition of serotonin reuptake in mammals. where A-B is -C=CH- or -CH-CH2-; R is H, or C1-C4; and HET is a bicyclic heteroaryl group optionally substituted with one or two substituents independently selected from the group consisting of H, halo, C1-C4 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxy, cyano, nitro, carboxamido, trifluoromethyl, or hydroxy; and pharmaceutically acceptable salts thereof.

  这项发明提供了式(I)的3-(双环杂芳基)-8-氮杂双环[3.2.1]辛烯和3-(双环杂芳基)-8-氮杂双环[3.2.1]辛烷，用于在哺乳动物中抑制血清素的再摄取。 其中 A-B为-C=CH-或-CH-CH2-； R为H，或C1-C4；和 HET为一个双环杂芳基团，可选地取代为从H、卤素、C1-C4烷基、C3-C6环烷基、C1-C4烷氧基、氰基、硝基、羧酰胺基、三氟甲基或羟基中独立选择的一个或两个取代基；以及其药学上可接受的盐。
• US6107307A
  申请人：——

  公开号：US6107307A

  公开（公告）日：2000-08-22
• [EN] NOVEL PROCESSES<br/>[FR] PROCEDES
  申请人：SMITHKLINE BEECHAM PLC

  公开号：WO2001014374A2

  公开（公告）日：2001-03-01

  Novel processes for the stereoselective preparation of exo- and endo- indolotropanes of formulae (IA) and (IB) wherein: R1 is hydrogen or (C¿1-6?)alkyl; R?2 and R3¿, which may be the same or different, are selected from the group consisting of hydrogen, halogen, cyano, (C¿1-6?)alkyl, (C3-7)cycloalkyl, (C1-6)alkoxy, halo(C1-6)alkyl, hydroxy, oxo, amino, mono- or di-(C1-6)alkylamino, acylamino, nitro, carboxy, (C1-6)alkoxycarbonyl, (C1-6)alkenyloxycarbonyl, (C1-6)alkoxycarbonyl(C1-6)alkyl, carboxy(C1-6)alkyl, (C1-6)alkylcarbonyloxy, carboxy(C1-6)alkyloxy, (C1-6)alkoxycarbonyl(C1-6)alkoxy, (C1-6)alkylthio, (C1-6)alkylsulphinyl, (C1-6)alkylsulphonyl, sulphamoyl, mono- and di-(C1-6)-alkylsulphamoyl, carbamoyl, mono- and di-(C1-6)alkylcarbamoyl, (C1-6)alkylsulphonamido, arylsulphonamido, aryl, aryl(C1-6)alkyl, aryl(C1-6)alkoxy, aryloxy, and heterocyclyl; Y is hydrogen, a nitrogen protecting group or an organic substituent; and Nq represents optional ring nitrogen atoms in positions 4, 5, 6, and 7; wherein q is O, 1 or 2.
• Inhibition of serotonin reuptake
  申请人：Eli Lilly and Company

  公开号：US06107307A1

  公开（公告）日：2000-08-22

  This invention provides 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]oct-2-enes and 3-(bicyclic heteroaryl)-8-azabicyclo[3.2.1]octanes which are useful for the inhibition of serotonin reuptake in mammals.

  本发明提供了对哺乳动物中的血清素再摄取有用的3-（双环杂环芳基）-8-氮杂双环[3.2.1]辛-2-烯和3-（双环杂环芳基）-8-氮杂双环[3.2.1]辛烷。