6-amino-2-fluorophenanthridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 6-amino-2-fluorophenanthridine
• 英文别名: 2-Fluorophenanthridin-6-amine
• 化学式: C₁₃H₉FN₂
• 分子量: 212.226
• InChiKey: RLIYRDWQJYCUFL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  苯乙醛 、 6-amino-2-fluorophenanthridine 在 1,2,3,4,5,6,7,8-八硫杂环辛烷 作用下， 以 环己烷 、 二甲基亚砜 为溶剂， 反应 8.0h， 以88%的产率得到C₂₁H₁₃FN₂
  参考文献：
  名称：

  无金属和无碱条件下咪唑并[1,2- f ]菲啶衍生物的合成及其抗癌活性

  摘要：

  在无金属和无碱条件下，采用原子经济策略，由菲啶-6-胺和醛经硫代环氧化环化反应合成了一系列咪唑并[1,2- f ]菲啶衍生物。在所有合成的衍生物中，化合物3d和3f的IC 50值分别为2.18±0.08和2.24μM±0.71μM。化合物3d对HT-29细胞具有最强的抑制活性，IC 50值为1.25μM±0.22μM，甚至比紫杉醇更强。

  DOI：

  10.1016/j.tetlet.2021.152908
• 作为产物：
  描述：

  2-溴-4-氟苯胺 在 bis-triphenylphosphine-palladium(II) chloride 、 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium phosphate 、 potassium acetate 作用下， 以 1,4-二氧六环 、 乙醇 、 水 、 甲苯 为溶剂， 反应 34.0h， 生成 6-amino-2-fluorophenanthridine
  参考文献：
  名称：

  마이크로웨이브를 이용하여 DMP를 리간드 구조로 포함한 동종리간드 이리듐 인광발광소재의 합성방법

  摘要：

  这项发明涉及一种基于DMP（二甲基苯基）配体的铱化合物的合成方法，可以以高产率和优异的工艺效率合成，（ⅰ）利用微波反应器，（ⅱ）利用“铱”异构体结构在反应过程中，可以获得明显提高产率的合成方法，相较于传统已知的产率。

  公开号：

  KR20180050795A

文献信息

• A single step synthesis of 6-aminophenanthridines from anilines and 2-chlorobenzonitriles
  作者：Fabienne Gug、Stéphane Bach、Marc Blondel、Jean-Michel Vierfond、Anne-Sophie Martin、Hervé Galons

  DOI：10.1016/j.tet.2004.03.062

  日期：2004.5

  Biologically active 6-aminophenanthridines were prepared in a single step procedure: Metal amides in liquid ammonia promoted the condensation of anilines with 2-chloro-benzonitriles. 6-Aminophenanthridines were isolated in moderate yield. (C) 2004 Elsevier Ltd. All rights reserved.
• Donnelly, Shileen; Grimshaw, James; Trocha-Grimshaw, Jadwiga, Journal of the Chemical Society. Perkin transactions I, 1993, # 14, p. 1557 - 1562
  作者：Donnelly, Shileen、Grimshaw, James、Trocha-Grimshaw, Jadwiga

  DOI：——

  日期：——
• CRIBLAGE DE MOLECULES A ACTIVITE ANTI-PRION : KITS, METHODES ET MOLECULES CRIBLEES
  申请人：CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)

  公开号：EP1551992B1

  公开（公告）日：2006-12-27
• Screening molecules with anti-prion activity: kits, methods and screened molecules
  申请人：Blondel Marc

  公开号：US20060172337A1

  公开（公告）日：2006-08-03

  The invention concerns screening molecules with anti-prion activity. More particularly, it concerns kits for screening molecules with anti-prion activity characterized in that they comprise in combination a [PSI+], phenotype yeast, an antibiogram and an agent for purifying prions at sub-efficient doses, said yeast including the adel-14 allele of the ADE1 gene and an inactivated ERG6 gene, the screening methods, and a family of molecules with anti-prion activity isolated by the inventive screen. The invention is applicable to anti-prion agents for producing medicines in particular for treating neurodegenerative diseases involving protein aggregates.
• SCREENING MOLECULES WITH ANTI-PRION ACTIVITY: KITS, METHODS AND SCREENED MOLECULES
  申请人：BLONDEL MARC

  公开号：US20110092483A1

  公开（公告）日：2011-04-21

  A kit and a method for identifying compounds having anti-prion activity are provided. The kit comprises a yeast of phenotype [PSI+]; an antibiogram; and a prion curing agent in a sub-effective dose, wherein the yeast has the adel-14 allele of the ADE1 gene and an inactivated ERG6 gene. Compounds and pharmaceutical compositions having anti-prion activity are also provided, which are useful for treating various neurodegenerative diseases, including polyglutamines expansion associated diseases; Huntington's disease; Kennedy disease; amyotrophic lateral sclerosis; cerebellous autosomic ataxies; dentalorubral-pallidoluysian atrophy; and spino-bulbar amyotrophy.