四氢-2-呋喃胺 | 127662-20-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氧唑烯
• 中文名称: 四氢-2-呋喃胺
• 英文名称: tetrahydrofurylamine
• 英文别名: amino-tetrahydrofuran；Tetrahydrofuran-2-amine；oxolan-2-amine
• CAS: 127662-20-8
• 化学式: C₄H₉NO
• 分子量: 87.1216
• InChiKey: KQOATKAFTRNONV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  N-[(2R)-5-bromopentan-2-yl]-4-chloro-N-[5-chloro-2-(oxan-2-yloxymethyl)phenyl]benzenesulfonamide 、 四氢-2-呋喃胺 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 18.0h， 生成
  参考文献：
  名称：

  Nitrogen-appended N-alkylsulfonamides as inhibitors of γ-secretase

  摘要：

  The synthesis and gamma-secretase inhibition data for a series of nitrogen-appended N-alkylsulfonamides (11-47) are described. Inhibition of brain A beta in transgenic mice was demonstrated by two of these compounds (23 and 44). (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.10.105

文献信息

• Solid-phase parallel synthesis of substituted dihydroimidazolyl dihydrobenzimidazol-2-ones
  作者：Achyuta N Acharya、John M Ostresh、Richard A Houghten

  DOI：10.1016/s0040-4020(02)00104-7

  日期：2002.3

  The solid-phase synthesis of substituted (4,5-dihydro-1H-imidazole-2-yl)-1,3-dihydro-2H-benzimidazol-2-ones is described. Following the amide reduction of a resin-bound (MBHA resin) amino acid, the primary amine was selectively acylated with 4-fluoro-3-nitrobenzoic acid. Treatment with POCl3, displacement of the fluoro group, and reduction of the nitro group generated an o-dianiline. Cyclization with

  取代的（4,5-二氢1所述的固相合成ħ咪唑-2-基）-1,3-二氢-2- ħ苯并咪唑-2-酮进行说明。酰胺键还原树脂结合的（MBHA树脂）氨基酸后，伯胺被4-氟-3-硝基苯甲酸选择性酰化。用POCl 3处理，取代氟基团和还原硝基基团生成邻二苯胺。用1，1-羰基二咪唑环化生成苯并咪唑酮类似物，随后将其用卤代烷N-烷基化。使用无水HF将化合物从固相支持物中裂解，并通过LC-MS以及1 H和13 C NMR光谱进行表征。
• Preparation and biodistribution of novel99mTc(CO)3-CNR complexes for myocardial imaging
  作者：Guiyang Hao、Jianying Zang、Boli Liu

  DOI：10.1002/jlcr.1151

  日期：——

  We evaluated lipophilicity and biodistribution of a series of 99mTc(CO)3-ether isonitrile complexes to determine whether different lipophilicity and structure of isonitrile ligands would improve the imaging properties of the radiopharmaceutical for the heart. Novel 99mTc(CO)3-MIBI analogs were prepared and analyzed by radio-HPLC, and their lipophilicity was determined. These new complexes could be bi- or tri-substituted in specified pH conditions like 99mTc(CO)3-MIBI. These new complexes exhibited low liver, lungs and blood uptake compared with [99mTc(CO)3(MIBI)3]+ though their heart uptake was not so high. Among these complexes, [99mTc(CO)3(EPI)2(OH2)]+ showed higher target to non-target ratios at 5 and 30 min post-injection than that of [99mTc(CO)3(MIBI)3]+. Copyright © 2007 John Wiley & Sons, Ltd.

  我们评估了一系列99mTc(CO)3-乙醚异腈复合物的亲脂性和生物分布，以确定异腈配体的不同亲脂性和结构是否能够改善心脏放射性药物的成像特性。我们制备了新型99mTc(CO)3-MIBI类似物，并通过放射-HPLC对其进行了分析，确定了它们的亲脂性。这些新复合物在特定的pH条件下可以像99mTc(CO)3-MIBI一样进行双取代或三取代。与[99mTc(CO)3(MIBI)3]+相比，这些新复合物在肝脏、肺部和血液中的摄取量较低，但心脏摄取量并不高。在这些复合物中，[99mTc(CO)3(EPI)2(OH2)]+在注射后5分钟和30分钟的目标与非目标比率高于[99mTc(CO)3(MIBI)3]+。版权所有 © 2007 John Wiley & Sons, Ltd.
• 4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES
  申请人：Jankowski Orion D.

  公开号：US20090118257A1

  公开（公告）日：2009-05-07

  Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

  本发明公开了治疗或抑制线粒体疾病的方法，例如弗里德雷希共济失调症（FRDA）、勒伯遗传性视神经病变（LHON）、线粒体肌病、脑病、乳酸中毒和中风（MELAS）、克恩斯-萨耶综合征（KSS），以及在该方法中有用的化合物，例如4-（对喹啉基）-2-羟基丁酰胺衍生物。本发明还公开了治疗其他疾病的方法和化合物，例如肌萎缩侧索硬化症（ALS）、亨廷顿病、帕金森病和广泛性发育障碍，如自闭症。本发明还公开了用于评估受试者代谢状态和治疗效果的能量生物标志物。本发明还公开了用于调节、规范或增强能量生物标志物的方法和有用于此类方法的化合物。
• 4-(p-quinonyl)-2-hydroxybutanamide derivatives for treatment of mitochondrial diseases
  申请人：Edison Pharmaceuticals, Inc.

  公开号：US07968746B2

  公开（公告）日：2011-06-28

  Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

  本发明公开了治疗或抑制线粒体疾病的方法，如弗里德赫氏共济失调症（FRDA）、勒伯遗传性视神经病变（LHON）、线粒体肌病、脑病、乳酸中毒和中风（MELAS）、基恩斯-塞尔综合症（KSS），以及在本发明方法中有用的化合物，如4-(p-喹啉基)-2-羟基丁酰胺衍生物。本发明还公开了治疗其他疾病，如肌萎缩性侧索硬化症（ALS）、亨廷顿病、帕金森病和广泛性发育障碍，如自闭症的方法和化合物。本发明还公开了用于评估受试者代谢状态和治疗效果的能量生物标志物。本发明还公开了调节、规范或增强能量生物标志物的方法，以及用于此类方法的化合物。
• NOVEL OXAZOLIDINONE DERIVATIVE AS CETP INHIBITOR, ITS PREPARATION METHOD, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
  申请人：DONG-A ST CO., LTD.

  公开号：US20160039804A1

  公开（公告）日：2016-02-11

  Disclosed are a novel oxazolidinone derivative exhibiting inhibitory activity against CETP, a preparation method thereof, and a pharmaceutical composition comprising the same. Exhibiting excellent inhibitory activity against CETP, the oxazolidinone derivative can be effectively applied to the prevention or treatment of various CETP enzyme activity- or HDL cholesterol level-related diseases such as dyslipidemia, atherosclerosis, and coronary heart disease.

  本发明公开了一种新型噁唑烷衍生物，该衍生物表现出对CETP的抑制活性，以及其制备方法和包含该衍生物的药物组合物。该噁唑烷衍生物表现出优异的CETP抑制活性，可有效应用于预防或治疗各种与CETP酶活性或高密度脂蛋白胆固醇水平相关的疾病，如血脂异常、动脉粥样硬化和冠心病。