1-acetyl-6-fluoroindolin-2-one | 651747-71-6

• 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: 1-acetyl-6-fluoroindolin-2-one
• 英文别名: 1-acetyl-6-fluoro-2-indolinone；1-acetyl-6-fluoro-1,3-dihydro-2H-indol-2-one；1-acetyl-6-fluoro-3H-indol-2-one
• CAS: 651747-71-6
• 化学式: C₁₀H₈FNO₂
• 分子量: 193.177
• InChiKey: DVFHFXFORJYWPC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.8
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-acetyl-6-fluoroindolin-2-one 、 4-(2-Boc-氨基乙基)苯甲酸 生成 1-acetyl-3-[1-hydroxy-1-(4-(N-tert-butoxycarbonyl-2-aminoethyl)phenyl)methylene]-6-fluoro-2-indolinone
  参考文献：
  名称：

  INDOLINE DERIVATIVES SUBSTITUTED IN THE 6 POSITION, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS

  摘要：

  本发明涉及6-位取代的吲哚酮衍生物，其化学式为其中R1至R6和X如权利要求1所定义，以及它们的互变异构体、对映异构体、非对映异构体、混合物和盐，特别是其生理上可接受的盐，具有有用的药理学性质，特别是在抑制各种受体酪氨酸激酶和内皮细胞以及各种肿瘤细胞的增殖方面，以及包含这些化合物的药物、它们的用途和制备方法。

  公开号：

  US20070004757A1
• 作为产物：
  描述：

  6-氟吲哚酮 在 乙酸酐 作用下， 反应 3.0h， 以61%的产率得到1-acetyl-6-fluoroindolin-2-one
  参考文献：
  名称：

  Indoline derivatives substituted in the 6 position, their preparation and their use as medicaments

  摘要：

  本发明涉及6-位取代的吲哚酮衍生物，其化学式为其中R1至R6和X如权利要求1中定义的，以及它们的互变异构体、对映体、顺反异构体、它们的混合物和它们的盐，特别是它们的生理上可接受的盐，具有有用的药理特性，特别是在抑制各种受体酪氨酸激酶的作用和对内皮细胞和各种肿瘤细胞的增殖方面，在包括这些化合物的药物、它们的使用和制备它们的方法方面。

  公开号：

  US20050043389A1

文献信息

• [EN] SALT FORMS OF A 6-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE DERIVATIVE, PROCESS FOR THEIR MANUFACTURE AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME<br/>[FR] FORMES DE SEL D'UN DÉRIVÉ DE 6-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDÈNE, PROCÉDÉ DE FABRICATION ET COMPOSITIONS PHARMACEUTIQUES LE CONTENANT
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2009092581A1

  公开（公告）日：2009-07-30

  The present invention relates to salt forms of the compound 4-[(Z)-[[4-[(dimethylaminoJmethyllphenyllaminolCe-fluoro-1,2-dihydro2-oxo-3H-indol-3-ylidene)methyl]-benzenepropanoic acid which are suitable for pharmaceutical development and to a process for their manufacture.

  本发明涉及化合物4-[(Z)-[[4-[(二甲氨基)甲基]苯基]氨基]-氟-1,2-二氢-2-氧-3H-吲哚-3-基亚甲基]-苯丙酸的盐形式，适用于药物开发，并涉及其制备方法。
• Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions
  申请人：Heckel Armin

  公开号：US20060194813A1

  公开（公告）日：2006-08-31

  The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R 1 to R 6 and X are defined as in claim 1 , the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

  本发明涉及一种在通式中6位取代的吲哚酮衍生物，其中R1至R6和X如权利要求1所定义，其互变异构体、对映异构体、顺反异构体、混合物及其盐，特别是其生理上可接受的盐，具有有价值的药理特性，特别是对各种受体酪氨酸激酶和内皮细胞以及各种肿瘤细胞的增殖具有抑制作用，包含这些化合物的制药组合物，它们的用途和制备过程。
• Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments
  申请人：Kley Joerg

  公开号：US20050054710A1

  公开（公告）日：2005-03-10

  The present invention relates to heterocyclically substituted indolinones of general formula wherein R 1 to R 5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

  本发明涉及一般式为的杂环取代吲哚酮 其中R1至R5和X的定义如权利要求1中所述，其互变异构体、对映异构体、混合物、前药及其盐，特别是具有有价值的药理学特性，特别是对各种受体酪氨酸激酶和环/ CDK复合物以及内皮细胞和各种肿瘤细胞的增殖具有抑制作用的生理上可接受的盐，包含这些化合物的制药组合物，它们的用途和制备它们的过程。
• Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US07169936B2

  公开（公告）日：2007-01-30

  The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.

  本发明涉及6-位取代的吲哚酮衍生物，其化学式为其中R1至R6和X如权利要求1所定义的那样，以及它们的互变异构体、对映异构体、顺反异构体、它们的混合物和它们的盐，特别是它们的生理上可接受的盐，具有有用的药理特性，特别是对各种受体酪氨酸激酶的抑制作用和对内皮细胞和各种肿瘤细胞的增殖的抑制作用，以及包含这些化合物的药物、它们的使用和它们的制备方法。
• Indoline derivatives substituted in the 6-position, their preparation and their use as medicaments
  申请人：Boehringer Ingelheim Pharma GmbH & Co. KG

  公开号：US07547703B2

  公开（公告）日：2009-06-16

  The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.

  本发明涉及6位取代的吲哚酮衍生物，其化学式如下：其中R1到R6和X的定义如权利要求1中所定义，以及它们的互变异构体、对映异构体、顺反异构体、混合物和盐，特别是其生理上可接受的盐，具有有用的药理特性，特别是在抑制各种受体酪氨酸激酶和内皮细胞以及各种肿瘤细胞增殖方面，包括这些化合物的药物、它们的用途和它们的制备方法。