5-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]indole | 146852-07-5

• 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: 5-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]indole
• 英文别名: 8-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]indole
• CAS: 146852-07-5
• 化学式: C₁₂H₁₃N
• 分子量: 171.242
• InChiKey: YSZRMPAYWRWLEH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  4.9
• 氢给体数：
  0
• 氢受体数：
  0

反应信息

• 作为产物：
  描述：

  1-allyl-7-methyl-1H-indole 以53%的产率得到5-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]indole
  参考文献：
  名称：

  一锅通过吲哚硼酸酯中的分子内烷基迁移反应获得环烷[1,2- a ]吲哚

  摘要：

  描述了一种新颖的一锅法，用于通过环状吲哚硼酸酯中的分子内烷基迁移反应制备环烷[1,2- a ]吲哚。发现NaOMe可作为成功的三烷基硼基保护基团来抵抗吲哚环C2上的锂化。用亲电试剂处理环状吲哚硼酸酯产生环烷-[1,2- a ]吲哚。

  DOI：

  10.1016/j.tet.2005.10.045

文献信息

• A novel synthetic use of trialkyl(indol-2-yl)borate for a “one-pot” synthesis of [a]-annelated indoles
  作者：Minoru Ishikura、Masanao Terashima

  DOI：10.1016/s0040-4039(00)61792-6

  日期：1992.11

  A novel one-pot procedure for [a]-annelated indole via cyclic trialkyl(indol-2-yl)borate is described.

  描述了通过环状三烷基（吲哚-2-基）硼酸酯用于[ α ]-退火的吲哚的新颖的一锅法。
• Inhibitors of protease-activated receptor-2
  申请人：Heptares Therapeutics Limited

  公开号：US10550089B2

  公开（公告）日：2020-02-04

  The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R1-R3 are as defined herein.

  本申请涉及某些取代咪唑和三唑化合物、含有它们的药物组合物以及使用它们的方法，包括治疗疼痛、肌肉骨骼炎症、神经炎性疾病、气道炎症、瘙痒、皮炎、结肠炎和相关疾病的方法。这些化合物为式（I）化合物，其中 X 是 N 或 CH，Z 和 Y 是 N 或 C（但两者都不是 N），R1-R3 如本文所定义。
• INHIBITORS OF PROTEASE-ACTIVATED RECEPTOR-2
  申请人：Heptares Therapeutics Limited

  公开号：US20190144394A1

  公开（公告）日：2019-05-16

  The present application relates to certain substituted imidazole and triazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions. The compounds are of Formula (I) where X is N or CH, Z and Y are N or C (but both not N) and R 1 -R 3 are as defined herein.
• A one-pot access to cycloalkano[1,2-a]indoles through an intramolecular alkyl migration reaction in indolylborates
  作者：Minoru Ishikura、Wataru Ida、Kazuo Yanada

  DOI：10.1016/j.tet.2005.10.045

  日期：2006.1

  protocol for the preparation of cycloalkano[1,2-a]indoles by way of an intramolecular alkyl migration reaction in cyclic indolylborates is described. NaOMe was found to act as a successful trialkylboryl-protecting group against to the lithiation at the C2 of the indole ring. Treatment of cyclic indolylborates with electrophiles produced cycloalkano-[1,2-a]indoles.

  描述了一种新颖的一锅法，用于通过环状吲哚硼酸酯中的分子内烷基迁移反应制备环烷[1,2- a ]吲哚。发现NaOMe可作为成功的三烷基硼基保护基团来抵抗吲哚环C2上的锂化。用亲电试剂处理环状吲哚硼酸酯产生环烷-[1,2- a ]吲哚。