Johnphos | 452068-71-2

• 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: Johnphos
• 英文别名: Biphenyl-3-yl-di-tert-butyl-phosphane；ditert-butyl-(3-phenylphenyl)phosphane
• CAS: 452068-71-2
• 化学式: C₂₀H₂₇P
• 分子量: 298.408
• InChiKey: ODSFBXNUHRLYKI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  21
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  0

反应信息

• 作为反应物：
  描述：

  Johnphos 、 金 、 nitrosonium tetrafluoroborate 、 乙腈 以 乙腈 为溶剂， 反应 9.0h， 以58%的产率得到Echavarren’s catalyst
  参考文献：
  名称：

  直接从金粉中简单地卤化和无银合成Echavarren催化剂†

  摘要：

  据报道，有一种简便的方法可直接从金粉中使用[ [Au（MeCN）（P t Bu 2 C 6 H 4 Ph-2）] [BF 4 ]（Echavarren's催化剂）制备具有合成价值的Au（I）配合物。NO] [BF 4 ]在乙腈中。该合成方法避免了单调乏味的常规合成过程中潜在存在的银或卤化物杂质，并且在其他方​​面已表明该催化剂或催化剂的性能适中。

  DOI：

  10.1039/c7dt04494a
• 作为试剂：
  描述：

  乙酰丙酸乙酯 在 potassium fluoride 、 lithium aluminium tetrahydride 、 Johnphos 、 偶氮二甲酸二异丙酯 、 polystyrene-bound PPh₃ 、 palladium diacetate 、 sodium hydride 、 碳酸氢钠 、 zinc(II) chloride 作用下， 以 四氢呋喃 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 27.5h， 生成 methyl 4-[2-[1-(diphenylmethyl)-2-methyl-5-phenyl-1H-indol-3-yl]ethoxy]benzoate
  参考文献：
  名称：

  Inhibition of Cytosolic Phospholipase A₂α: Hit to Lead Optimization

  摘要：

  Compound I was previously reported to be a potent inhibitor of cPLA,(x in both artificial monomeric substrate and cell-based assays. However, I was inactive in whole blood assays previously used to characterize cyclooxygenase and lipoxygenase inhibitors. The IC(50) of 1 increased dramatically with cell number or lipid/detergent concentration. In an attempt to insert an electrophilic ketone between the indole and benzoic acid moieties, we discovered that increasing the distance between the two moieties gave a compound with activity in the GLU (7-hydroxycoumarinyl-gamma-linolenate) micelle assay, which contains lipid and detergent. Extensive structure-activity relationship work around this lead identified a potent pharmacophore for cPLA a inhibition. The IC(50)s between the GLU micelle and rat whole blood assays correlated highly. No correlation was found for other parameters, including lipophilicity or acidity of the required acid functionality. Compounds 25, 39, and 94 emerged as potent, selective inhibitors of cPLA(2)alpha and represent well-validated starting points for further optimization.

  DOI：

  10.1021/jm0507882

文献信息

• [EN] HETEROCYCLIC COMPOUNDS, IN PARTICULAR 2-OXO-4,4,5,5,6,6,7,7-OCTAHYDROBENZOXAZOLE DERIVATIVES, AND THEIR USE AS ANTIBACTERIAL COMPOUNDS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES, EN PARTICULIER DÉRIVÉS DE 2-OXO -4,4,5,5,6,6,7,7-OCTAHYDROBENZOXAZOLE, ET LEUR UTILISATION EN TANT QUE COMPOSÉS ANTIBACTÉRIENS
  申请人：REDX PHARMA PLC

  公开号：WO2017137744A1

  公开（公告）日：2017-08-17

  This invention relates to antibacterial drug compounds containing a bicyclic core, typically a bicycle in which one of the rings is an oxazolidinone. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the compounds in treating bacterial infections and in methods of treating bacterial infections.

  这项发明涉及含有双环核心的抗菌药物化合物，通常是其中一个环是噁唑烷酮的双环。它还涉及抗菌药物化合物的药物配方。它还涉及化合物在治疗细菌感染和治疗细菌感染方法中的用途。
• Novel high affinity thiophene-based and furan-based kinase ligands
  申请人：Deng Yongqi

  公开号：US20070043045A1

  公开（公告）日：2007-02-22

  Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.

  描述了抑制细胞周期依赖性激酶2（CDK-2）的抑制剂、包括这些抑制剂的组合物，以及使用这些抑制剂和抑制剂组合物的方法。这些抑制剂和包括它们的组合物对于治疗疾病或疾病症状是有用的。该发明还提供了制备CDK-2抑制剂化合物的方法、抑制CDK-2的方法，以及治疗疾病或疾病症状的方法。
• [EN] A PROCESS FOR THE REDUCTION OF A TERTIARY PHOSPHINE OXIDE TO THE CORRESPONDING TERTIARY PHOSPHINE IN THE PRESENCE OF A CATALYST AND USE OF A TERTIARY PHOSPHINE FOR REDUCING A TERTIARY PHOSPHINE OXIDE IN THE PRESENCE OF A CATALYST<br/>[FR] PROCÉDÉ DE RÉDUCTION D'UN OXYDE DE PHOSPHINE TERTIAIRE EN LA PHOSPHINE TERTIAIRE CORRESPONDANTE EN PRÉSENCE D'UN CATALYSEUR, ET UTILISATION D'UNE PHOSPHINE TERTIAIRE POUR RÉDUIRE UN OXYDE DE PHOSPHINE TERTIAIRE EN PRÉSENCE D'UN CATALYSEUR
  申请人：CHROMAFORA AB

  公开号：WO2011123037A1

  公开（公告）日：2011-10-06

  A process for the conversion of a tertiary phosphine oxide to the corresponding tertiary phosphine comprising reacting said tertiary phosphine oxide with a reducing tertiary phosphine, in the presence of a catalyst that catalyzes the conversion.

  一种将三级膦氧转化为对应的三级膦的方法，包括在催化剂的存在下，将所述三级膦氧与还原三级膦反应，以催化转化。
• Process for preparing tertiary phosphines
  申请人：——

  公开号：US20030229240A1

  公开（公告）日：2003-12-11

  The invention relates to a process for synthesizing tertiary phosphines by reacting halophosphines with organomagnesium compounds in the presence of copper compounds and optionally of salts.

  本发明涉及一种合成三级膦化合物的方法，通过在铜化合物和可选盐的存在下，将卤化膦化合物与有机镁化合物反应。
• METHOD FOR PRODUCING AROMATIC COMPOUND
  申请人：Sumitomo Chemical Company, Limited

  公开号：US20150322199A1

  公开（公告）日：2015-11-12

  A method is provided for producing an aromatic compound, including a step of mixing a compound represented by formula (A) and a compound represented by formula (B): in the presence of at least one phosphine compound selected from the group consisting of a phosphine represented by formula (C) and a phosphonium salt represented by formula (D): a base, a palladium compound, and an aprotic organic solvent.

  提供一种生产芳香化合物的方法，包括以下步骤：在至少一种磷化合物的存在下，将公式（A）表示的化合物和公式（B）表示的化合物混合；所述磷化合物从以下组中选择：公式（C）表示的膦化合物和公式（D）表示的膦盐；加入碱、钯化合物和无质子有机溶剂。