2-氟-7-硝基芴 | 1806-25-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 中文名称: 2-氟-7-硝基芴
• 英文名称: 2-fluoro-7-nitro-fluorene
• 英文别名: 2-Fluor-7-nitro-fluoren；2-Fluoro-7-nitrofluorene；2-fluoro-7-nitro-9H-fluorene
• CAS: 1806-25-3
• 化学式: C₁₃H₈FNO₂
• 分子量: 229.21
• InChiKey: ZGVSZORIRFNOCF-UHFFFAOYSA-N

物化性质

• 熔点：
  201-204 °C(lit.)
• 沸点：
  378.4±35.0 °C(Predicted)
• 密度：
  1.394±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S26,S36
• 危险类别码：
  R36/37/38
• 海关编码：
  2904909090

反应信息

• 作为反应物：
  描述：

  2-氟-7-硝基芴 在 calcium chloride 、 锌 作用下， 以 乙醇 为溶剂， 生成 2-Fluor-7-cyan-fluoren
  参考文献：
  名称：

  Berkovic,S., Israel Journal of Chemistry, 1963, vol. 1, p. 1 - 11

  摘要：

  DOI：
• 作为产物：
  描述：

  2-溴-5-硝基苄醇 在 palladium diacetate 、 PPA 作用下， 以 1,4-二氧六环 为溶剂， 生成 2-氟-7-硝基芴
  参考文献：
  名称：

  Synthesis and biological activities of aryl-ether-, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT-2

  摘要：

  Excitatory amino acid transporters (EAATs) play a pivotal role in maintaining glutamate homeostasis in the mammalian central nervous system, with the EAAT-2 subtype thought to be responsible for the bulk of the glutamate uptake in forebrain regions. A complete elucidation of the functional role of EAAT-2 has been hampered by the lack of potent and selective pharmacological tools. In this study, we describe the synthesis and biological activities of novel aryl-ether, biaryl-, and fluorene-aspartic acid and diaminopropionic acid analogs as potent inhibitors of EAAT-2. Compound (16) represents one of the most potent (IC50 = 85 +/- 5 nM) and selective inhibitors of EAAT-2 identified to date. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.08.003

文献信息

• COMPOSITIONS AND METHODS FOR BIOLOGICAL SAMPLE STORAGE
  申请人：Whitney Scott E.

  公开号：US20110081363A1

  公开（公告）日：2011-04-07

  Compositions and methods are disclosed for substantially dry storage at ambient or elevated temperatures of biological samples such as nucleic acids, proteins and cells in a form from which the samples can be substantially recovered, using a dissolvable or dissociable dry storage matrix comprising a borate composition and a stabilizer as disclosed, such as any of a number of zwitterionic stabilizers.

  本发明公开了一种用于在常温或升高温度下实现生物样品（如核酸、蛋白质和细胞）的基本干燥储存的组合物和方法，所述生物样品可以在其中以基本恢复的形式被恢复，使用可溶解或可分解的干燥储存基质，该基质包含硼酸盐组合物和稳定剂，例如多种带电离的稳定剂之一。
• [EN] NOVEL ASPARTYLAMIDE INHIBITORS OF EXCITATORY AMINO ACID TRANSPORTERS<br/>[FR] NOUVEAUX INHIBITEURS D'ASPARTYLAMIDE DE TRANSPORTEURS D'ACIDE AMINÉ EXCITATEURS
  申请人：UNIV MONTANA

  公开号：WO2013134241A1

  公开（公告）日：2013-09-12

  The compounds of the invention are inhibitors of excitatory amino acid transporters (EAAT) that penetrate the blood-brain barrier to access the central nervous system. The compounds of the invention follow the structural formula: or a salt, ester or prodrug thereof, wherein X is a halogen, such as fluorine, or a radionuclide, such as fluorine-18. The compounds and methods described herein can be used for the treatment of, e.g., neurodegenerative disorders (e.g., amyotrophic lateral sclerosis), ischemia, spinal cord injury, and traumatic brain injury in a patient (e.g., a human). The invention further provides compounds and methods for the synthesis and use of radiographic tracers to diagnose and follow the progression of such disorders.

  本发明的化合物是兴奋性氨基酸转运体（EAAT）的抑制剂，能穿过血脑屏障进入中枢神经系统。本发明的化合物遵循以下结构式：或其盐、酯或前药，其中X是卤素，如氟，或放射性核素，如氟-18。本文描述的化合物和方法可用于治疗神经退行性疾病（例如肌萎缩侧索硬化症）、缺血、脊髓损伤和创伤性脑损伤等患者（例如人类）。本发明还提供了用于合成和使用放射示踪剂以诊断和追踪这些疾病进展的化合物和方法。
• The Michael Reaction of Fluoro-substituted-9,9′-Bifluorenylidenes and -Fluorenes, and the Syntheses of Some Related Compounds
  作者：Masahiro Minabe、Akio Tanaka、Masahiro Wakui、Kazuo Suzuki

  DOI：10.1246/bcsj.44.1614

  日期：1971.6

  The Michael reaction of fluoro-substituted 9,9′-bifluorenylidenes and fluorenes was carried out; the normal addition products, fluoro-substituted tribiphenylenepropanes, were obtained, but no abnormal product was isolated. Some new fluoro-substituted-fluorenes, -9,9′-bifluorenylidenes, -9,9′-bifluorenyls and -α,δ-dibiphenylenebutadienes, were synthesized. The structures of the fluoro-substituted t

  进行了氟取代的9,9'-二芴基与芴的迈克尔反应；得到了正常的加成产物，氟取代的亚联苯丙烷，但没有分离出异常产物。合成了一些新的氟取代芴、-9,9'-联芴、-9,9'-联芴和-α,δ-二联亚苯基丁二烯。氟取代的亚联苯丙烷的结构通过 9-锂硫芴和 9-溴-9,9'-二芴基的锂-卤素互变反应得到证实。氟取代的亚联苯丙烷的热解得到氟取代或非氟取代的-9,9'-二芴基、-9,9'-二芴基、-芴和-芴酮。差示扫描量热法应用于氟取代的 9,9'-二芴基和三联苯丙烷。
• Mechanism-based inactivation of N-arylhydroxamic acid N,O-acyltransferase by 7-substituted-N-hydroxy-2-acetamidofluorenes
  作者：Virginia C. Marhevka、Nancy A. Ebner、Russell D. Sehon、Patrick E. Hanna

  DOI：10.1021/jm00379a005

  日期：1985.1

  N-Arylhydroxamic acid N,O-acyltransferase (AHAT) catalyzes the transfer of the N-acetyl group from N-arylhydroxamic acids to arylamines. In the absence of an arylamine acceptor, AHAT catalyzes the conversion of N-arylhydroxamic acids to reactive electrophilic intermediates that become irreversibly bound to cellular nucleophiles, including those present on AHAT itself. As part of an investigation of

  N-芳基异羟肟酸N，O-酰基转移酶（AHAT）催化N-乙酰基从N-芳基异羟肟酸转移至芳基胺。在不存在芳基胺受体的情况下，AHAT催化N-芳基异羟肟酸转化为反应性亲电中间体，该中间体不可逆地与细胞亲核试剂（包括AHAT本身上存在的亲核试剂）结合。作为AHAT催化生物活化过程研究的一部分，合成了N-羟基-2-乙酰氨基芴（1）的一系列7-取代类似物，并在体外评估了部分纯化的仓鼠肝AHAT制剂的底物和灭活剂。所有这些化合物在AHAT催化的4-氨基偶氮苯（AAB）的反乙酰化中均充当乙酰基供体，并且它们都是AHAT的失活剂。失活过程表现出明显的一级动力学，而7-甲氧基化合物表现出最大的失活速率常数。定量结构活性分析为该系列化合物使AHAT失活涉及带正电荷的物种这一概念提供了支持。与AHAT和N-芳基异羟肟酸的培养混合物中包括谷胱甘肽，半胱氨酸，蛋氨酸，磷酸鸟苷和tRNA等亲核捕获剂的实验结果表明，从酶
• COMPOSITIONS FOR STABILIZING DNA, RNA AND PROTEINS IN BLOOD AND OTHER BIOLOGICAL SAMPLES DURING SHIPPING AND STORAGE AT AMBIENT TEMPERATURES
  申请人：Whitney Scott E.

  公开号：US20120052572A1

  公开（公告）日：2012-03-01

  Compositions and methods are disclosed for substantially liquid, gel, suspension, slurry, semisolid and/or colloid storage of biological samples following admixture with the herein disclosed storage composition, permitting substantial recovery of biological activity following storage without refrigeration. In certain embodiments, unfractionated blood or tissue samples may be stored without refrigeration for weeks, months or years in a form that permits recovery of intact DNA, RNA or protein components following the storage period.

  本发明揭示了一种用于生物样品的基本液体、凝胶、悬浮液、泥浆、半固态和/或胶体储存的组合物和方法，该组合物与所述储存组合物混合后，可以在不需要冷藏的情况下储存生物活性，并在储存期后实现生物活性的大量恢复。在某些实施例中，未分离的血液或组织样品可以以一种形式储存数周、数月或数年，以便在储存期后恢复完整的DNA、RNA或蛋白质组分。