2-fluoro-4-(dimethylamino)benzaldehyde | 1524-07-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-fluoro-4-(dimethylamino)benzaldehyde
• 英文别名: 2-Fluor-4-dimethylamino-benzaldehyd；4-dimethylamino-2-fluorobenzaldehyde；4-(Dimethylamino)-2-fluorobenzaldehyde
• CAS: 1524-07-8
• 化学式: C₉H₁₀FNO
• mdl: MFCD16656996
• 分子量: 167.183
• InChiKey: HTPRYYQFLDDHCT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  12
• 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：
  20.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-fluoro-4-(dimethylamino)benzaldehyde 在 sodium tetrahydroborate 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 26.5h， 生成 N'-[2,6-Dichloro-4-(4-dimethylamino-2-fluoro-benzylamino)-phenyl]-N,N-dimethyl-formamidine
  参考文献：
  名称：

  N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents

  摘要：

  The synthesis of a series of N2-[4-[(arylmethyl)amino]-2, 6-dichlorophenyl]-N1,N1-dimethylformamidines that caused marked blood pressure lowering and/or diuresis in spontaneously hypertensive rats (SHR) is reported. Diuretic activity was not always associated with acute antihypertensive activity. Central nervous system effects, most notably sedation, were observed. Compound 9d, which lowered arterial blood pressure 37 mmHg in SHR when dosed at 100 mg/kg, was further evaluated in chronic hypertensive dogs because of apparent minimal CNS effects. A reduction in arterial blood pressure of 32 mmHg at 1.0 mg/kg during a 6-h postdosing interval was observed. This response was unrelated to alpha- or beta-adrenergic blockade, angiotensin I antagonism, or neuronal or ganglionic blockade. CNS effects were also observed.

  DOI：

  10.1021/jm00378a030
• 作为产物：
  描述：

  1-(二甲基氨基)-3-氟苯 、 N,N-二甲基甲酰胺 在 水 、 三氯氧磷 作用下， 生成 2-fluoro-4-(dimethylamino)benzaldehyde
  参考文献：
  名称：

  N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents

  摘要：

  The synthesis of a series of N2-[4-[(arylmethyl)amino]-2, 6-dichlorophenyl]-N1,N1-dimethylformamidines that caused marked blood pressure lowering and/or diuresis in spontaneously hypertensive rats (SHR) is reported. Diuretic activity was not always associated with acute antihypertensive activity. Central nervous system effects, most notably sedation, were observed. Compound 9d, which lowered arterial blood pressure 37 mmHg in SHR when dosed at 100 mg/kg, was further evaluated in chronic hypertensive dogs because of apparent minimal CNS effects. A reduction in arterial blood pressure of 32 mmHg at 1.0 mg/kg during a 6-h postdosing interval was observed. This response was unrelated to alpha- or beta-adrenergic blockade, angiotensin I antagonism, or neuronal or ganglionic blockade. CNS effects were also observed.

  DOI：

  10.1021/jm00378a030

文献信息

• NEAR INFRARED FLUOROGEN AND FLUORESCENT ACTIVATING PROTEINS FOR IN VIVO IMAGING AND LIVE-CELL BIOSENSING
  申请人：Carnegie Mellon University

  公开号：US20140243509A1

  公开（公告）日：2014-08-28

  Tissue slices and whole organisms offer substantial challenges to fluorescence imaging. Autofluorescence and absorption via intrinsic chromophores, such as flavins, melanin, and hemoglobins, confound and degrade output from all fluorescent tags. An “optical window,” farther red than most autofluorescence sources and in a region of low hemoglobin and water absorbance, lies between 650 and 900 nm. This valley of relative optical clarity is an attractive target for fluorescence-based studies within tissues, intact organs, and living organisms. Novel fluorescent tags were developed herein, based upon a genetically targeted fluorogen activating protein and cognate fluorogenic dye that yields emission with a peak at 733 nm exclusively when complexed as a “fluoromodule”. This tool improves substantially over previously described far-red/NIR fluorescent proteins in terms of brightness, wavelength, and flexibility by leveraging the flexibility of synthetic chemistry to produce novel chromophores.

  组织切片和整个生物体对荧光成像提出了重大挑战。自发荧光和内在色素（如黄酮，黑色素和血红蛋白）的吸收会干扰和降解所有荧光标记的输出。在650到900纳米之间，比大多数自发荧光源更远的“光学窗口”处于低血红蛋白和水吸收区域内，是组织，完整器官和活体内荧光研究的有吸引力的目标。本文开发了一种新型荧光标记，基于基因定向荧光原活化蛋白和相应的荧光原染料，仅当复合为“荧光模块”时，才产生峰值为733纳米的发射。通过利用合成化学的灵活性来生产新的色素，该工具在亮度，波长和灵活性方面显着优于先前描述的远红外/近红外荧光蛋白。
• RADIOPROTECTOR COMPOUNDS AND RELATED METHODS
  申请人：Martin Roger Francis

  公开号：US20100022557A1

  公开（公告）日：2010-01-28

  The invention relates to radioprotectors of formula (I), processes for their preparation and their use in protecting biological materials from radiation damage. In diagnostic and therapeutic radiology, particularly in cancer radiotherapy, the radioprotectors of the present invention may be used to protect certain normal tissues or structures from radiation damage. The radioprotectors of formula (I) may also have uses in decreasing the effects of irradiation in non-medical scenarios, both civil and military.

  该发明涉及式(I)的辐射防护剂，其制备过程以及它们在保护生物材料免受辐射损伤方面的应用。在诊断和治疗放射学中，特别是在癌症放射治疗中，本发明的辐射防护剂可用于保护某些正常组织或结构免受辐射损伤。式(I)的辐射防护剂还可以用于减少非医学场景中的辐射影响，包括民用和军事领域。
• WO2008/74091
  申请人：——

  公开号：——

  公开（公告）日：——
• MEYER, W. E.;TOMCUFCIK, A. S.;CHAN, P. S.;EMMA, J. E., J. MED. CHEM., 1984, 27, N 12, 1705-1710
  作者：MEYER, W. E.、TOMCUFCIK, A. S.、CHAN, P. S.、EMMA, J. E.

  DOI：——

  日期：——
• US4360466A
  申请人：——

  公开号：US4360466A

  公开（公告）日：1982-11-23