4-溴-2-氟苯甲酰胺乙酯 | 749927-82-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-溴-2-氟苯甲酰胺乙酯
• 英文名称: 4-bromo-N-ethyl-2-fluorobenzamide
• CAS: 749927-82-0
• 化学式: C₉H₉BrFNO
• mdl: MFCD09928893
• 分子量: 246.079
• InChiKey: WRCAXTFEUQRZDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.222
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2924299090

SDS

4-溴-2-氟苯甲酰胺乙酯MSDS英文版

反应信息

• 作为反应物：
  描述：

  4-溴-2-氟苯甲酰胺乙酯 在 磺酰氯 、 palladium diacetate 、 caesium carbonate 、 三苯基膦 作用下， 以 1,4-二氧六环 、 二甲基亚砜 、 甲苯 为溶剂， 反应 7.0h， 生成 2-ethyl-6-{8-[(4′-fluoro[1,1′-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-1,2-benzothiazol-3(2H)-one hydrogen chloride
  参考文献：
  名称：

  Optimization and biological evaluation of imidazopyridine derivatives as a novel scaffold for γ-secretase modulators with oral efficacy against cognitive deficits in Alzheimer’s disease model mice

  摘要：

  Gamma-secretase modulators (GSMs) selectively lower amyloid-beta 42 (A beta 42) and are therefore potential disease-modifying drugs for Alzheimer's disease (AD). Here, we report the discovery of imidazopyridine derivatives as GSMs with oral activity on not only A beta 42 levels but also cognitive function. Structural optimization of the biphenyl group and pyridine-2-amide moiety of compound 1a greatly improved GSM activity and rat microsomal stability, respectively. 5-{8-[(3,4'-Difluoro[1,1'-biphenyl]-4-yl)methoxy]-2-methylimidazo[1,2-a]pyridin3-yl}-N-methylpyridine-2-carboxamide (1o) showed high in vitro potency and brain exposure, induced a robust reduction in brain A beta 42 levels, and exhibited undetectable inhibition of cytochrome p450 enzymes. Moreover, compound 1o showed excellent efficacy against cognitive deficits in AD model mice. These findings suggest that compound 1o is a promising candidate for AD therapeutics.

  DOI：

  10.1016/j.bmc.2020.115455
• 作为产物：
  描述：

  乙胺 、 4-溴-2-氟苯甲酸 在 氯化亚砜 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 3.33h， 以90%的产率得到4-溴-2-氟苯甲酰胺乙酯
  参考文献：
  名称：

  [EN] 6-PHENYL- OR 6-(PYRIDIN-3-YL)INDAZOLE DERIVATIVES AND METHODS OF USE
  [FR] DÉRIVÉS DE 6-PHÉNYL OU 6-(PYRIDIN-3-YL)INDAZOLE ET PROCÉDÉS D'UTILISATION

  摘要：

  公式(I)的化合物以及药用可接受的盐、酯、酰胺或放射性标记形式，其中R1、R2、R3、R4、R5、R6和X如说明书所述，可用于治疗通过Tropomysin受体激酶（Trk）预防或改善的状况或疾病。公开了制造这些化合物的方法。还公开了公式(I)化合物的药物组合物，以及使用这些化合物和组合物的方法。

  公开号：

  WO2015112445A1

文献信息

• 6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use
  申请人：ABBVIE INC.

  公开号：US20160376240A1

  公开（公告）日：2016-12-29

  Compounds of formula (I) and pharmaceutically acceptable salts, esters, amides, or radiolabelled forms thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and X are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by Tropomysin receptor kinases (Trk). Methods for making the compounds are disclosed. Also disclosed are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

  公式(I)的化合物以及药用可接受的盐、酯、酰胺或放射性标记形式，其中R1、R2、R3、R4、R5、R6和X如说明书中所定义，可用于治疗通过Tropomysin受体激酶（Trk）预防或改善的状况或疾病。公开了制备这些化合物的方法。还公开了公式(I)化合物的药物组合物，以及使用这些化合物和组合物的方法。
• Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
  申请人：Borchardt Allen

  公开号：US20050176701A1

  公开（公告）日：2005-08-11

  The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R 1 and R 2 , are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

  这项发明涉及公式1的化合物，以及其药学上可接受的盐、溶剂化合物、前药和代谢物，其中W、Z、R1和R2如本文所定义。该发明还涉及通过给哺乳动物施用公式1的化合物来治疗丙型肝炎病毒的方法，以及用于治疗这类疾病的含有公式1化合物的药物组合物。该发明还涉及制备公式1化合物的方法。
• [EN] HIGHLY SELECTIVE C-MET INHIBITORS AS ANTICANCER AGENTS<br/>[FR] INHIBITEURS HAUTEMENT SÉLECTIFS DE C-MET UTILISÉS COMME AGENTS ANTICANCÉREUX
  申请人：CROWN BIOSCIENCE INC TAICANG

  公开号：WO2014032498A1

  公开（公告）日：2014-03-06

  Disclosed are novel nitrogen-containing, heterocyclic, c-Met inhibitor compounds, processes for their preparation and formulations thereof. The compounds are useful as therapeutical agents for the inhibition, regulation, and control of c-Met kinase signal pathway, and useful for treating in a subject a cell proliferative disorder or disorders mediated by c-Met.

  本文披露了新型含氮、杂环、c-Met抑制剂化合物，其制备方法和配方。这些化合物可用作治疗剂，用于抑制、调节和控制c-Met激酶信号通路，并用于治疗受c-Met介导的主体细胞增殖紊乱或疾病。
• INHIBITORS OF HEPATITIS C VIRUS RNA-DEPENDENT RNA POLYMERASE, AND COMPOSITIONS AND TREATMENTS USING THE SAME
  申请人：Borchardt Allen

  公开号：US20060189681A1

  公开（公告）日：2006-08-24

  The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, solvates, prodrugs and metabolites thereof, wherein W, Z, R 1 and R 2 , are as defined herein. The invention also relates to methods of treating Hepatitis C virus in mammals by administering the compounds of formula 1, and to pharmaceutical compositions for treating such disorders, which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.

  本发明涉及式1的化合物以及其药学上可接受的盐、溶剂合物、前药和代谢物，其中W、Z、R1和R2如本文所定义。本发明还涉及通过给哺乳动物投予式1的化合物来治疗丙型肝炎病毒的方法，以及包含式1的化合物的用于治疗此类疾病的制药组合物。本发明还涉及制备式1的化合物的方法。
• Biphenyloxyacetic Acid Derivatives for the Treatment of Respiratory Disease
  申请人：Luker Timothy Jon

  公开号：US20080132480A1

  公开（公告）日：2008-06-05

  The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1 , as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

  本发明涉及式(I)的取代苯氧基乙酸，其中变量如权利要求书1所定义，作为治疗呼吸系统疾病的有用药物化合物，以及包含它们的药物组合物和它们的制备方法。