4-chloro-5-methoxyisatin | 33234-38-7

• 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: 4-chloro-5-methoxyisatin
• 英文别名: 4-chloro-5-methoxy-1H-indole-2,3-dione；4-Chlor-5-methoxyisatin；4-chloro-5-methoxy-indole-2,3-dione；4-chloro-5-methoxy-indoline-2,3-dione；4-Chlor-5-methoxy-indolin-2,3-dion
• CAS: 33234-38-7
• 化学式: C₉H₆ClNO₃
• 分子量: 211.605
• InChiKey: UAMMYAPYQZBSSZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  55.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-chloro-5-methoxyisatin 在 三溴化硼 作用下， 生成 (4-chloro-5-hydroxy-1H-indole-2,3-dione)
  参考文献：
  名称：

  [EN] INDOLINONE HYDRAZIDES AS C-MET INHIBITORS
  [FR] HYDRAZIDES D'INDOLINONE UTILISES EN TANT QU'INHIBITEURS DU RECEPTEUR C-MET

  摘要：

  公开号：

  WO2005005378A3
• 作为产物：
  描述：

  N-(3-氯-4-甲氧基苯基)乙酰胺 在 硫酸 、 水 作用下， 生成 4-chloro-5-methoxyisatin
  参考文献：
  名称：

  AN ANTIMALARIAL ALKALOID FROM HYDRANGEA. XV. SYNTHESIS OF 5-, 6-, 7-, AND 8-DERIVATIVES WITH TWO IDENTICAL SUBSTITUENTS

  摘要：

  DOI：

  10.1021/jo01135a015

文献信息

• Tetracyclic compounds as c-Met inhibitors
  申请人：Vojkovsky Tomas

  公开号：US20050014755A1

  公开（公告）日：2005-01-20

  The present invention relates to compounds of the Formulae (I) and (II), wherein R 1 —R 10 and G are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer.

  本发明涉及式（I）和（II）化合物，其中R1-R10和G在此定义，并且它们的药学上可接受的盐。这些化合物调节c-Met的活性，因此预计在预防和治疗c-Met相关疾病如癌症方面有用。
• Indolinone hydrazides as c-Met inhibitors
  申请人：Koenig Marcel

  公开号：US20060009493A1

  公开（公告）日：2006-01-12

  The present invention relates to compounds of the formulae (I)-(XII), wherein R 1 -R 71 , A, B, X, Y, G, L and Z are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer.

  本发明涉及式(I)-(XII)的化合物，其中R1-R71、A、B、X、Y、G、L和Z在此定义，并且它们的药学上可接受的盐。这些化合物调节c-Met的活性，因此预计在预防和治疗与c-Met相关的疾病，如癌症方面有用。
• 2-Benzazepine compounds, processes for their preparation and pharmaceutical compositions containing them
  申请人：SMITHKLINE BECKMAN CORPORATION

  公开号：EP0002624A1

  公开（公告）日：1979-06-27

  This invention concerns a process for preparing 2- benzazepine compounds which inhibit the enzyme phenylethanolamine N-methyltransferase and show activity in reducing anxiety. The compounds produced have substituents in the 8- and/or 9-positions, and optionally substituents in the 1- and 2-positions. The compounds are prepared by debenzylating an appropriately substituted N-benzyl 2-benzazepine with optional acylation and reduction, or with optional ozidation and alkylation of the debenzylated product to introduce 2- and 1-position substituents, respectively. Acid addition salts of the compounds are also prepared.

  本发明涉及一种制备 2-苯并氮杂卓化合物的工艺，该化合物可抑制苯乙醇胺 N-甲基转移酶，并具有减轻焦虑的活性。所制备的化合物在 8 位和/或 9 位上有取代基，在 1 位和 2 位上也有取代基。这些化合物的制备方法是将适当取代的 N-苄基 2-苯并氮杂卓进行去苄基化，然后进行任选的酰化和还原，或对去苄基化产物进行任选的羰基化和烷基化，以分别引入 2 位和 1 位取代基。还可制备这些化合物的酸加成盐。
• Oxindole-Based Inhibitors of Cyclin-Dependent Kinase 2 (CDK2):  Design, Synthesis, Enzymatic Activities, and X-ray Crystallographic Analysis
  作者：H. Neal Bramson、John Corona、Stephen T. Davis、Scott H. Dickerson、Mark Edelstein、Stephen V. Frye、Robert T. Gampe、Phil A. Harris、Anne Hassell、William D. Holmes、Robert N. Hunter、Karen E. Lackey、Brett Lovejoy、Michael J. Luzzio、Val Montana、Warren J. Rocque、David Rusnak、Lisa Shewchuk、James M. Veal、Duncan H. Walker、Lee F. Kuyper

  DOI：10.1021/jm010117d

  日期：2001.12.1

  Two closely related classes of oxindole-based compounds, 1H-indole-2,3-dione 3-phenylhydrazones and 3-(anilinomethylene)-1,3-dihydro-2H-indol-2-ones, were shown to potently inhibit cyclin-dependent kinase 2 (CDK2). The initial lead compound was prepared as a homologue of the 3-benzylidene-1,3-dihydro-2H-indol-2-one class of kinase inhibitor. Crystallographic analysis of the lead compound bound to CDK2 provided the basis for analogue design. A semiautomated method of ligand docking was used to select compounds for synthesis, and a number of compounds with low nanomolar inhibitory activity versus CDK2 were identified. Enzyme binding determinants for several analogues were evaluated by X-ray crystallography. Compounds in this series inhibited CDK2 with a potency similar to 10-fold greater than that for CDK1. Members of this class of inhibitor cause an arrest of the cell cycle and have shown potential utility in the prevention of chemotherapy-induced alopecia.
• Varma; Singh, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 1990, vol. 29, # 6, p. 578 - 581
  作者：Varma、Singh

  DOI：——

  日期：——