N-(2-aminophenyl)indoline

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N-(2-aminophenyl)indoline
• 英文别名: 2-(1H-indolinyl)aniline；1-(aminophenyl)indoline；2-(2,3-dihydro-indol-1-yl)-aniline；1-(2-Aminophenyl)-indolin；2-(Indolin-1-yl)aniline；2-(2,3-dihydroindol-1-yl)aniline
• 化学式: C₁₄H₁₄N₂
• mdl: MFCD08699289
• 分子量: 210.279
• InChiKey: FTCUPLCIWYYZLT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.142
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-(2-aminophenyl)indoline 、 2-溴-4'-甲基苯乙酮 在 三氟乙酸 作用下， 以 氯仿 为溶剂， 反应 4.0h， 以86%的产率得到
  参考文献：
  名称：

  一锅，两组分级联反应通过骨架多样地合成吲哚并重氮和二氮杂骨架

  摘要：

  已经探索了一种快速新颖的策略来合成结构多样的吲哚稠合的重氮辛和二氮杂卓衍生物。一种基于底物的3-氨基吲哚甲基/吲哚啉苯甲酸甲酯的多样化方法，与Pictet-Spengler反应和三个不同的反应级联反应，提供了吲哚二氮杂和吲哚喹喔啉。吲哚二唑胺的形成过程是通过初始缩合，然后进行分子内烷基化而进行的。

  DOI：

  10.1021/acs.orglett.5b03481

文献信息

• 7-[4-(substituted
  申请人：Hoechst Marion Roussel Inc.

  公开号：US05536717A1

  公开（公告）日：1996-07-16

  There are disclosed various compounds of the formula below, ##STR1## where the parameters X, Y, R.sub.1 and R.sub.2 are as defined in the specification which are useful as antidepressant and analgesic agents.

  下面的公式揭示了各种化合物，##STR1## 其中参数X、Y、R.sub.1和R.sub.2如规范中定义的那样，这些化合物可用作抗抑郁和镇痛剂。
• HETEROCYCLIC TRPML1 AGONISTS
  申请人：Libra Therapeutics, Inc.

  公开号：EP3821947A1

  公开（公告）日：2021-05-19

  The invention relates to a compound of formula (I) or a stereoisomer thereof, or a salt of any of the foregoing and to processes for its preparation. The compounds of formula (I) are useful in the treatment TRPML1- mediated disorders or diseases.

  该发明涉及公式(I)的化合物或其立体异构体，或任何上述化合物的盐，以及其制备的过程。公式(I)的化合物在治疗TRPML1介导的疾病或疾病中有用。
• Benzo[b]pyrrolo[3,2,1-jk][1,4]benzodiazepines having dopamine receptor
  申请人：Hoechst-Roussel Pharmaceuticals Inc.

  公开号：US04663453A1

  公开（公告）日：1987-05-05

  The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio, benzyl, benzyl in which the phenyl group is substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio or CO.sub.2 R.sub.11 wherein R.sub.11 is lower alkyl, or a pharmaceutically acceptable acid salt thereof.

  本发明涉及式为##STR1##的苯并吡咯苯并二氮杂环己烷和喹诺苯并二氮杂环己烷，其中X和Y可以相同也可以不同，每个都是氢、卤素、CF.sub.3、低烷基、低烷氧基、低烷硫基和低烷基磺酰基，p和q是独立的1或2；当R.sub.2与R.sub.3结合形成--(CH.sub.2).sub.m --CH.sub.2 --基团或--CH.dbd.CH--基团时，R.sub.1为氢；当R.sub.1与R.sub.2结合形成--(CH.sub.2).sub.m --CH.sub.2 --基团或--CH.dbd.CH--基团时，R.sub.3为氢；m为1或2；R.sub.4为NR.sub.5 R.sub.6，其中R.sub.5为氢或低烷基，R.sub.6为氢、低烷基或(CH.sub.2).sub.n NR.sub.7 R.sub.8的基团，其中R.sub.7和R.sub.8为低烷基，n为2或3，##STR2##其中R.sub.9为低烷基，##STR3##其中R.sub.10为CH.sub.2 CH.sub.2 OH、低烷基、苯基、卤代苯基、CF.sub.3、低烷氧基或低烷硫基的取代苯基、苄基、卤代苄基、CF.sub.3、低烷氧基或低烷硫基的取代苄基或CO.sub.2 R.sub.11，其中R.sub.11为低烷基，或其药学上可接受的酸盐。
• Indolo-,1,2-dihydroindolo-, and 1,2,6,7-tetrahydroindolo [1,7-ab][1,5]
  申请人：American Hoechst Corporation

  公开号：US04186199A1

  公开（公告）日：1980-01-29

  What is disclosed are ##STR1## wherein X is hydrogen, halogen or trifluoromethyl; Y is hydrogen, halogen or trifluoromethyl; R is hydrogen, loweralkyl, cycloalkyl, phenyl, halophenyl, furyl, pyridinyl, 4-methylpiperazin-1-ylethyl or phenylloweralkyl; R.sup.1 is hydrogen; n and m are independently 0 or 1, but n is not 0 when m is 1, and the bonds between ring positions 1 and 2 and between positions 6 and 7 are respectively saturated when n and m are 1 and are unsaturated when n and m are 0; pharmaceutically acceptable acid addition salts thereof; methods of preparing said compounds; pharmaceutical compositions including said compounds; methods of treatment using the compounds; and intermediates therefor. These compounds are useful as analgesic and anti-inflammatory agents, as well as intermediates for the preparation of other pharmaceutically active compounds.

  所披露的是##STR1##其中X为氢、卤素或三氟甲基；Y为氢、卤素或三氟甲基；R为氢、低碳基、环烷基、苯基、卤代苯基、呋喃基、吡啶基、4-甲基哌嗪-1-乙基或苯基低碳基；R.sup.1为氢；n和m独立地为0或1，但当m为1时，n不为0，当n和m为1时，1和2号环位置之间的键和6和7号位置之间的键分别饱和，当n和m为0时，它们是不饱和的；药学上可接受的酸盐；制备这些化合物的方法；包括这些化合物的制药组合物；使用这些化合物的治疗方法；以及其中间体。这些化合物可用作镇痛和抗炎剂，以及其他药学活性化合物的制备中间体。
• Benzopyrrolobenzodiazepines and quinobenzodiazepines
  申请人：Hoechst-Roussel Pharmaceuticals Inc.

  公开号：US04723007A1

  公开（公告）日：1988-02-02

  The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio, benzyl, benzyl in which the phenyl group is substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio or CO.sub.2 R.sub.11 wherein R.sub.11 is lower alkyl, or a pharmaceutically acceptable acid salt thereof.

  本发明涉及公式##STR1##中的苯并吡咯苯并二氮杂环和喹诺苯并二氮杂环，其中X和Y可以相同也可以不同，每个都是氢、卤素、CF.sub.3、低烷基、低烷氧基、低烷硫基和低烷基磺酰基，p和q独立地为1或2; 当R.sub.2与R.sub.3结合形成--(CH.sub.2).sub.m --CH.sub.2--基团或--CH.dbd.CH--基团时，R.sub.1为氢; 当R.sub.1与R.sub.2结合形成--(CH.sub.2).sub.m --CH.sub.2--基团或--CH.dbd.CH--基团时，R.sub.3为氢; m为1或2; R.sub.4为NR.sub.5R.sub.6，其中R.sub.5为氢或低烷基，R.sub.6为氢、低烷基或(CH.sub.2).sub.nNR.sub.7R.sub.8的基团，其中R.sub.7和R.sub.8为低烷基，n为2或3，##STR2##其中R.sub.9为低烷基，##STR3##其中R.sub.10为CH.sub.2CH.sub.2OH、低烷基、苯基、被卤素、CF.sub.3、低烷基氧基或低烷硫基取代的苯基、苄基、苄基中苯基被卤素、CF.sub.3、低烷基氧基或低烷硫基取代或CO.sub.2R.sub.11，其中R.sub.11为低烷基，或其药学上可接受的酸盐。