4-硝基苯基 2-重氮基-3,3,3-三氟丙酸酯 | 59733-94-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 4-硝基苯基 2-重氮基-3,3,3-三氟丙酸酯
• 中文别名: 4-硝基苯基2-重氮基-3,3,3-三氟丙酸酯
• 英文名称: 2-diazo-3,3,3-trifluoropropionic acid p-nitrophenyl ester
• 英文别名: p-nitrophenyl 2-diazo-3,3,3-trifluoropropionate；4-Nitrophenyl-2-diazo-3,3,3-trifluoropropionate；(4-nitrophenyl) 2-diazo-3,3,3-trifluoropropanoate
• CAS: 59733-94-7
• 化学式: C₉H₄F₃N₃O₄
• 分子量: 275.144
• InChiKey: YHJZWYNRTYKWEC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  74.1
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  4-硝基苯基 2-重氮基-3,3,3-三氟丙酸酯 、 [(S)-5-Amino-5-(3-{tert-butoxycarbonyl-[4-(tert-butoxycarbonyl-{3-[(S)-2-heptanoylamino-3-(4-methoxy-phenyl)-propionylamino]-propyl}-amino)-butyl]-amino}-propylcarbamoyl)-pentyl]-carbamic acid tert-butyl ester 在 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 48.0h， 生成 [(S)-5-(3-{tert-Butoxycarbonyl-[4-(tert-butoxycarbonyl-{3-[(S)-2-heptanoylamino-3-(4-methoxy-phenyl)-propionylamino]-propyl}-amino)-butyl]-amino}-propylcarbamoyl)-5-(2-diazo-3,3,3-trifluoro-propionylamino)-pentyl]-carbamic acid tert-butyl ester
  参考文献：
  名称：

  Structure-binding relation of philanthotoxins from nicotinic acetylcholine receptor binding assay

  摘要：

  Philanthotoxins are noncompetitive inhibitors of the nicotinic acetylcholine receptor and the Various glutamate receptors. Analogues carrying photoaffinity labels, fluorine atoms for solid-state NMR studies of ligand/receptor interaction, and large head groups such as porphyrins and planar bulky aromatic rings (BIG analogues) for clarifying mode of entry and orientation of analogues in receptors have been synthesized, assayed against the nicotinic acetylcholine receptor, and brief comments are given for the assay results. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0968-0896(97)00137-5

文献信息

• Substituted N, N-disubstituted diamino compounds useful for inhibiting cholesteryl ester transfer protein activity
  申请人：——

  公开号：US20020120011A1

  公开（公告）日：2002-08-29

  The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted diamines. A preferred specific N,N-disubstituted diamine is the compound: 1

  这项发明涉及替代多环芳基和杂环芳基的三级杂烷基胺化合物，可用作胆固醇酯转移蛋白（CETP；血浆脂质转移蛋白-I）的抑制剂，以及用于治疗动脉粥样硬化和其他冠状动脉疾病的化合物、组合物和方法。首选的三级杂烷基胺化合物是取代的N,N-二取代二胺。首选的具体N,N-二取代二胺化合物是：1
• PRODRUG COMPOSITIONS, PRODRUG NANOPARTICLES, AND METHODS OF USE THEREOF
  申请人：Washington University

  公开号：US20160279060A1

  公开（公告）日：2016-09-29

  The present invention encompasses prodrug compositions, nanoparticles comprising one or more prodrugs, and methods of use thereof.

  本发明涵盖了前药组合物、包含一种或多种前药的纳米粒子，以及其使用方法。
• [EN] NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF<br/>[FR] COMPOSITIONS D'ACIDE NUCLÉIQUE-POLYPEPTIDE ET UTILISATIONS DE CELLES-CI
  申请人：AVIDITY BIOSCIENCES LLC

  公开号：WO2019071028A1

  公开（公告）日：2019-04-11

  Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.

  本文披露了包含与修饰的多核苷酸分子和聚合物结合基团的组合物和药物配方。本文还描述了利用包含与多核苷酸分子和聚合物结合基团共轭的组合物或药物配方治疗癌症的方法。
• Chloroquine combination drugs and methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20070060499A1

  公开（公告）日：2007-03-15

  This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.

  这项发明揭示了氯喹偶联活性药剂的组合物，包括其制备方法。先前的技术已经表明，以足够高浓度给予氯喹作为游离药物，可以增强细胞内体内各种药剂从细胞内体释放到细胞质中。这些组合物的目的是在传递活性药剂的相同部位提供受控量的氯喹，从而减少所需的总剂量。这些组合物包括将氯喹物质直接或通过各种药用载体物质偶联到活性药剂。载体物质包括多糖、合成聚合物、蛋白质、胶束和其他用于在体内携带和释放氯喹组合物以产生治疗效果的物质。这些组合物还可以包括用于携带和释放活性药剂以用于治疗或其他医疗用途的生物可降解连接。该发明还揭示了与靶向分子偶联的载体组合物，用于将氯喹物质和活性药剂定位传递到它们的作用部位。
• Chloroquine coupled nucleic acids and methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20060040879A1

  公开（公告）日：2006-02-23

  This invention discloses compositions and methods for preparing chloroquine-coupled nucleic acid compositions. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the nucleic acid needs to be released, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a nucleic acid directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

  本发明披露了制备氯喹偶联核酸组合物的组成和方法。先前的研究表明，以足够高的浓度给予氯喹作为自由药物，可以增强细胞内体内各种物质从内体泡中释放到细胞质中。这些组合物的目的是在核酸需要释放的同一位置提供受控量的氯喹，从而降低所需的总剂量。该组合物包括直接或通过各种药物载体物质偶联的氯喹物质和核酸。载体物质包括多糖、合成聚合物、蛋白质、胶束和其他用于在体内携带和释放氯喹组合物以达到治疗效果的物质。该组合物还可以包括生物可降解连接来携带和释放用于治疗或其他医疗用途的核酸。本发明还披露了偶联到靶向分子的核酸载体组合物，用于将核酸传递到其作用位置。