(3-nitrobenzyl)-triphenyl-phosphonium

• 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: (3-nitrobenzyl)-triphenyl-phosphonium
• 英文别名: (3-nitrobenzyl)triphenylphosphonium；<3-Nitro-benzyl>-triphenylphosphonium；(m-Nitro-benzyl)-triphenyl-phosphonium；(3-Nitrophenyl)methyl-triphenylphosphanium
• 化学式: C₂₅H₂₁NO₂P
• 分子量: 398.421
• InChiKey: BDVNCRCGKMFCMO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.3
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-formyl-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester 、 (3-nitrobenzyl)-triphenyl-phosphonium 在 lithium hydroxide 作用下， 以 甲醇 为溶剂， 以87%的产率得到5-[2-(3-nitrophenyl)-vinyl]-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid methyl ester
  参考文献：
  名称：

  [EN] AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS
  [FR] DÉRIVÉS AZA-INDOLIQUES UTILISÉS COMME INHIBITEURS DE MULTIPLES KINASES

  摘要：

  本发明涉及式(I)化合物和/或其药用可接受的增加盐、溶剂化物、对映异构体、非对映异构体，以及它们的混合物。因此，本发明的主题还包括式(I)化合物的制备、用途，特别是在抑制涉及多种疾病（如癌症或免疫系统疾病）的蛋白激酶方面的用途。

  公开号：

  WO2014102377A1
• 作为产物：
  描述：

  三苯基膦 、 3-硝基溴苄 以 甲苯 为溶剂， 以100%的产率得到(3-nitrobenzyl)-triphenyl-phosphonium
  参考文献：
  名称：

  [EN] AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS
  [FR] DÉRIVÉS AZA-INDOLIQUES UTILISÉS COMME INHIBITEURS DE MULTIPLES KINASES

  摘要：

  本发明涉及式(I)化合物和/或其药用可接受的增加盐、溶剂化物、对映异构体、非对映异构体，以及它们的混合物。因此，本发明的主题还包括式(I)化合物的制备、用途，特别是在抑制涉及多种疾病（如癌症或免疫系统疾病）的蛋白激酶方面的用途。

  公开号：

  WO2014102377A1

文献信息

• Reaction between Peroxynitrite and Triphenylphosphonium-Substituted Arylboronic Acid Isomers: Identification of Diagnostic Marker Products and Biological Implications
  作者：Adam Sikora、Jacek Zielonka、Jan Adamus、Dawid Debski、Agnieszka Dybala-Defratyka、Bartosz Michalowski、Joy Joseph、Richard C. Hartley、Michael P. Murphy、Balaraman Kalyanaraman

  DOI：10.1021/tx300499c

  日期：2013.6.17

  (TPP) group on the reaction between ONOO– and mitochondria-targeted arylboronate isomers (o-, m-, and p-MitoPhB(OH)2). Results from the electron paramagnetic resonance (EPR) spin-trapping experiments unequivocally showed the presence of a phenyl radical intermediate from meta and para isomers, and not from the ortho isomer. The yield of o-MitoPhNO2 formed from the reaction between o-MitoPhB(OH)2 and ONOO–

  芳族硼酸与过氧亚硝酸盐 (ONOO – ) 快速反应生成酚类作为主要产物。该反应用于监测细胞系统中 ONOO的形成。此前，我们提出ONOO -和芳基硼酸酯(PhB(OH) 2 ) 之间的反应产生酚类产物（主要途径）和自由基对PhB(OH) 2 O •– ··· • NO 2（次要途径）。[西科拉，A.等。( 2011 )化学。水库。毒理学。24 , 687-697]。在这项研究中，我们研究了庞大的三苯基鏻 (TPP) 基团对 ONOO与线粒体靶向芳基硼酸酯异构体（o-、m-和p -MitoPhB(OH) 2）之间反应的影响。电子顺磁共振 (EPR) 自旋捕获实验的结果明确表明存在来自间位和对位异构体的苯基自由基中间体，而不是来自邻位异构体。o -MitoPhNO 2的产率由它们之间的反应形成o -MitoPhB(OH) 2和 ONOO –没有被苯基自由基清除剂减少，这表明o -MitoPhB(OH)
• PYRIDONE COMPOUND
  申请人：Kamikubo Takashi

  公开号：US20100179137A1

  公开（公告）日：2010-07-15

  [Solving Means] The present inventors have conducted extensive studies on an EP4 receptor agonist, and as a result, found that a novel pyridone compound characterized in that the 1-position in the pyridone ring is substituted with a group having an acidic group such as a carboxyl group and the 6-position is bonded with an aromatic ring group via lower alkyl, lower alkylene, ether, or thioether, has an excellent EP4 receptor agonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor agonistic action and a blood flow increasing action in the hindlimb of a rat, it is useful as a pharmaceutical, in particular, an agent for treating peripheral arterial occlusive disease.

  【解决方法】本发明者对EP4受体激动剂进行了广泛的研究，并发现一种新型吡啶酮化合物，其特征在于吡啶酮环中的1位被取代为具有酸性基团（如羧基）的基团，而6位则通过较低的烷基、烷基烷基、醚或硫醚与芳香环基团结合，具有极好的EP4受体激动作用，从而完成了本发明。由于本发明的化合物在大鼠后肢具有出色的EP4受体激动作用和增加血流的作用，因此可用作制药用途，特别是治疗周围动脉闭塞性疾病的药物。
• AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS
  申请人：ORIBASE PHARMA

  公开号：US20150353539A1

  公开（公告）日：2015-12-10

  The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.

  本发明涉及以下式(I)的化合物和/或其药学上可接受的加合盐、溶剂化物、对映体、非对映异构体以及它们的混合物。因此，本发明的主题还包括制备式(I)化合物，它们的用途，特别是在抑制蛋白激酶方面的用途，这些蛋白激酶例如与许多疾病有关，如癌症或免疫系统紊乱。
• NONIMMUNOSUPPRESSIVE CYCLOSPORINE ANALOGUE MOLECULES
  申请人：Hegmans Alexander

  公开号：US20130190223A1

  公开（公告）日：2013-07-25

  The compounds of the present invention are non-immunosupressive cyclosporine analogue molecules that are able to bind cyclophilin. Said compounds include a modified side chain of amino acid I of cyclosporin A, consisting of an oxyalkyl having substituents R′, R1 and R2, where R′ is H or Acetyl; R1 is a saturated or unsaturated straight chain or branched aliphatic carbon chain; and R2 may be a hydrogen; a unsubstituted, N substituted or NN disubstituted amide; a N substituted or unsubstituted acyl protected amine; a carboxylic acid; a N substituted or unsubstituted amine; a nitrile; a ester; a ketone; a hydroxy, dihydroxy, trihydroxy or polyhydroxy alkyl; or a substituted or unsubstituted aryl.
• CYCLOSPORINE ANALOGUE MOLECULES MODIFIED AT AMINO ACID 1 AND 3
  申请人：Hegmans Alexander

  公开号：US20140142033A1

  公开（公告）日：2014-05-22

  Analogues of cyclosporin-A are disclosed comprising modifications of the substituents as the positions of amino acids 1 and 3, according to the following Formula. The disclosed compounds include compounds having affinity for cyclophilin, including cyclophilin-A, and reduced immunosuppressivity in comparison with cyclosporin-A and analogs thereof modified solely at position 1.