diphenyl phosphite | 102-10-3

• 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: diphenyl phosphite
• 英文别名: Phosphorous diphenyl ester；diphenyl hydrogen phosphite
• CAS: 102-10-3
• 化学式: C₁₂H₁₁O₃P
• 分子量: 234.191
• InChiKey: FYOYCZHNDCCGCE-UHFFFAOYSA-N

物化性质

• 沸点：
  150-152 °C(Press: 1 Torr)
• 密度：
  1.2318 g/cm3
• 熔点：
  25 °C

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  16
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.7
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  diphenyl phosphite 在 四丁基溴化铵 、 magnesium oxide 、 三苯基膦 、 2,3-二氯-5,6-二氰基-1,4-苯醌 作用下， 以 二氯甲烷 为溶剂， 生成 diphenyl [bromo(4-iodophenyl)methyl]phosphonate
  参考文献：
  名称：

  β-吡咯修饰的卟啉的合成及其掺入DNA

  摘要：

  描述了合成各种β-吡咯基官能化卟啉及其与2'-脱氧尿苷和DNA共价结合的合成方法。钯（0）催化的Sonogashira和铜（I）催化的Huisgen 1,3-偶极环加成反应用于将卟啉插入2'-脱氧尿苷和DNA的结构。卟啉插入具有4个胞嘧啶5'末端序列的单链CT寡核苷酸的中间被显示会触发pH和温度依赖性i-基序结构的形成。卟啉的插入还导致单链嘌呤-嘧啶序列的聚集，可通过在90°C加热5分钟来解离。在适当的互补链存在下，形成了平行三链体和反平行双链体。根据修改，卟啉被放置在双链体的主要和次要槽中，并用作双链体和三链体的凸出的插入插入物。通常，观察到具有卟啉修饰的三链体形成寡核苷酸（TFO）链的平行三链体的热稳定性，而反平行双链体则不稳定。这些结果将根据分子模型计算的结果进行比较和讨论。

  DOI：

  10.1002/chem.201003200
• 作为产物：
  描述：

  Diphenyl phosphorochloridite 在 甲醇 作用下， 生成 diphenyl phosphite
  参考文献：
  名称：

  Petrov,K.A. et al., Journal of general chemistry of the USSR, 1962, vol. 32, # 11, p. 3650 - 3653

  摘要：

  DOI：
• 作为试剂：
  描述：

  齐多夫定 、 三乙胺 在 吡啶 、 diphenyl phosphite 作用下， 以 吡啶 、 水 为溶剂， 反应 2.0h， 以840 mg的产率得到triethylammonium 3'-azido-3'-deoxythymidine 5'-phosphite
  参考文献：
  名称：

  Synthesis, in Vitro Anti-Breast Cancer Activity, and Intracellular Decomposition of Amino Acid Methyl Ester and Alkyl Amide Phosphoramidate Monoesters of 3‘-Azido-3‘-deoxythymidine (AZT)

  摘要：

  We report the synthesis and anticancer activity of a series of AZT phosphoramidate monoesters containing amino acid methyl ester (3a-11a) and N-alkyl amide (3b-11b, 9c-9f) moieties. The aromatic amino acid methyl esters were found to be more cytotoxic than the aliphatic analogues toward MCF-7 cells (human pleural effusion breast adenocarcinoma cell line). A marked stereochemical preference for the L-amino acid stereochemistry was also observed in MCF-7 cells. There was no consistent enhancement of cytotoxicity of the methyl amides over the corresponding methyl esters. AZT and the two AZT aromatic amino acid methyl ester phosphoramidates 8a and 9a were found to be more cytotoxic toward MCF-7 cells than to CEM cells (human T-cell lymphoblastic leukemia). The selective cytotoxicity toward MCF-7 cells may be associated with greater intracellular levels of phosphoramidate monoester and/or phosphorylated AZT.

  DOI：

  10.1021/jm000110g

文献信息

• [EN] NOVEL SYNTHETIC OLIGOMERS OF NEISSERIA MENINGITIS SEROGROUP X AND PROCESS OF PREPARING THEM<br/>[FR] NOUVEAUX OLIGOMÈRES SYNTHÉTIQUES DU SÉROGROUPE X DE NEISSERIA MENINGITIDIS ET LEUR PROCÉDÉ DE PRÉPARATION
  申请人：MSD WELLCOME TRUST HILLEMAN LAB PVT LTD

  公开号：WO2015128797A1

  公开（公告）日：2015-09-03

  The present invention relates to synthesis of novel higher oligomers and process of preparing the same. In particular the present invention relates to the chemical synthesis of oligomers of Neisseria meningitidis serogroup X ('hereinafter Men-X), more particularly tetramer. The present invention provides Men-X capsular oligomers obtained from synthetic pathway using purified saccharides of specific chain length and provides said novel oligomers as candidates for the development of conjugate vaccine against bacterial meningitis caused due to Men-X infections.

  本发明涉及合成新型高聚物以及制备该高聚物的方法。具体来说，本发明涉及化学合成脑膜炎球菌X群（以下简称Men-X）寡聚体，更具体地说是四聚体。本发明提供了通过使用特定链长的纯化糖类合成途径获得的Men-X包膜寡聚体，并将这些新型寡聚体作为开发针对Men-X感染引起的细菌性脑膜炎的结合疫苗候选物。
• [EN] FLUORESCENT SUBSTRATES FOR POLY(ADP-RIBOSYL) HYDROLASES<br/>[FR] SUBSTRATS FLUORESCENTS POUR POLY(ADP-RIBOSYL) HYDROLASES
  申请人：UNIV ILLINOIS

  公开号：WO2020055753A1

  公开（公告）日：2020-03-19

  The post-translational modification (PTM) and signaling molecule poly(ADP-ribose) (PAR) has an impact on diverse biological processes. PTM is regulated by a series of ADP-ribosyl glycohydrolases (PARG enzymes) that cleave polymers and/or liberate monomers from their protein targets. Disclosed herein is a substrate for monitoring PARG activity, TFMU-ADPr, which directly reports on total PAR hydrolase activity via release of a fluorophore; this substrate has excellent reactivity, generality, stability, and usability. A second substrate, TFMU-IDPr, selectively reports on PARG activity only from the enzyme ARH3. Use of these probes in whole-cell lysate experiments has revealed a mechanism by which ARH3 is inhibited by cholera toxin. TFMU-ADPr and TFMU-IDPr are versatile tools for assessing small-molecule inhibitors in vitro and probing the regulation of ADP-ribosyl catabolic enzymes.

  翻译结果：翻译后修饰（PTM）和信号分子聚腺苷二磷酸核糖（PAR）对多种生物过程产生影响。PTM受一系列ADP核糖水解酶（PARG酶）调控，这些酶从它们的蛋白靶标中切割聚合物和/或释放单体。本文披露了一种用于监测PARG活性的底物，TFMU-ADPr，它通过释放荧光团直接报告总PAR水解酶活性；该底物具有出色的反应性、普适性、稳定性和可用性。第二种底物TFMU-IDPr，只选择性地报告来自酶ARH3的PARG活性。在全细胞裂解液实验中使用这些探针揭示了一种由霍乱毒素抑制ARH3的机制。TFMU-ADPr和TFMU-IDPr是评估体外小分子抑制剂和探究ADP核糖降解酶调控的多功能工具。
• NOVEL STING AGONISTS
  申请人：Venenum Biodesign, LLC

  公开号：US20200131209A1

  公开（公告）日：2020-04-30

  The present invention provides compounds of Formula I′: wherein , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

  本发明提供了式I′的化合物： 其中 , W, X, Y, Z, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 和R 5 如本文所定义，或其立体异构体、互变异构体、药学上可接受的盐、前药酯或溶剂化合物形式，其中所有变量均如本文所定义。这些化合物能有效调节STING蛋白，因此可用作治疗或预防受STING激动影响的疾病的药物。
• [EN] NOVEL TRIAZOLE AND OXAZOLE COMPOUNDS AS TRANSFORMING GROWTH FACTOR (TGF) INHIBITOR<br/>[FR] NOUVEAUX COMPOSES DE TRIAZOLE ET D'OXAZOLE, INHIBITEURS DU FACTEUR DE CROISSANCE TRANSFORMANT
  申请人：PFIZER PROD INC

  公开号：WO2004026863A1

  公开（公告）日：2004-04-01

  Novel thiazole derivatives of formula I a - c, intermediates fo their preparation, pharmaceutical compositions containing them and their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor ('TGF')-βsignaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

  描述了公式I a - c的新噻唑衍生物，其制备的中间体，含有它们的药物组合物以及它们的药用。本发明的化合物是转化生长因子（'TGF'）-β信号通路的有效抑制剂。它们在治疗各种与TGF相关的疾病状态中非常有用，例如癌症和纤维化疾病。
• Novel fused heteroaromatic compounds as transforming growth factor (TGF) inhibitors
  申请人：Pfizer Inc

  公开号：US20040176390A1

  公开（公告）日：2004-09-09

  Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-&bgr; signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.

  描述了新型融合杂芳化合物，包括其衍生物，以及用于其制备的中间体，含有它们的药物组合物以及它们的药用。本发明的化合物是转化生长因子（“TGF”）-β信号通路的有效抑制剂。它们在治疗各种与TGF相关的疾病状态中非常有用，包括癌症和纤维化疾病。