3-(benzyloxymethyl)-6-methyl-1,4-dioxane-2,5-dione

• 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-(benzyloxymethyl)-6-methyl-1,4-dioxane-2,5-dione
• 英文别名: (3S,6S)-3-benzyloxymethyl-6-methyl-1,4-dioxane-2,5-dione；(3S,6S)-3-methyl-6-(phenylmethoxymethyl)-1,4-dioxane-2,5-dione
• 化学式: C₁₃H₁₄O₅
• 分子量: 250.251
• InChiKey: BJUHVQXYPKQGSY-ONGXEEELSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  61.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  (S)-3-(benzyloxy)-2-hydroxypropanoic acid 在 N,N-二异丙基乙胺 、 potassium iodide 作用下， 以 二氯甲烷 、 丙酮 为溶剂， 生成 3-(benzyloxymethyl)-6-methyl-1,4-dioxane-2,5-dione 、 3-(benzyloxymethyl)-6-methyl-1,4-dioxane-2,5-dione
  参考文献：
  名称：

  使用无催化剂、全氟芳基叠氮化物介导的快速施陶丁格反应合成碳水化合物接枝的糖聚合物。

  摘要：

  糖聚合物在研究聚糖-凝集素相互作用、作为药物输送载体以及调节与蛋白质的相互作用方面变得越来越重要。这些糖聚合物的合成仍然是一项具有挑战性和严格性的工作。在这方面，高效的点击反应，铜（I）催化的炔烃叠氮化物环加成，不仅因其效率而且因其对附加碳水化合物基团的耐受性而被广泛应用。然而，该方法的一个显着缺点是使用了难以完全去除的重金属催化剂，并且最终对生物系统有毒。在这项工作中，我们提出了利用温和且无催化剂的全氟苯基叠氮化物（PFPA）介导的施陶丁格反应合成碳水化合物接枝的糖聚合物。采用这种策略，通过在室温下在 DMSO 中搅拌 PFAA 功能化的 PLA 与膦衍生的 Man 或 MH，将甘露糖 (Man) 和麦芽七糖 (MH) 接枝到可生物降解的聚乳酸 (PLA) 上，一小时内完成。通过 1H-NMR、 19F-NMR、 31P-NMR 和 FTIR 对糖聚合物进行了表征。

  DOI：

  10.3390/molecules24010157

文献信息

• PARTICULATE DRUG DELIVERY
  申请人：Cheng Jianjun

  公开号：US20080248126A1

  公开（公告）日：2008-10-09

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates which are useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications. The invention additionally provides certain drug-polymer and drug-oligomer conjugates which are useful in the preparation of particles for delivery of the drug in vivo. The invention also provides nanoparticles of this invention prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  本发明提供了一种有效制备药物-聚合物（或寡聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以在体内传递药物进行治疗应用。本发明还提供了某些药物-聚合物和药物-寡聚物共轭物，该共轭物可用于制备体内药物传递的微粒。本发明还提供了通过使用本发明的药物-聚合物/寡聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或寡聚物的聚合过程中形成的，其中药物被用作引发单体聚合形成聚合物和/或寡聚物的引发剂。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）的存在下开环聚合环状单体形成的。该方法特别适用于与含有一个或多个羟基或硫醇基团的药物和其他化学物质形成聚合物/寡聚物共轭物。
• PARTICULATE DRUG DELIVERY METHODS
  申请人：The Board of Trustees of the University of Illinois

  公开号：US20150314006A1

  公开（公告）日：2015-11-05

  Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

  提供了用于高效制备药物-聚合物（或低聚物）共轭物的方法，该方法可用于制备微粒和纳米粒子，以便在体内传递药物进行治疗应用。本发明还提供了使用本发明的药物-聚合物/低聚物共轭物制备的纳米粒子。药物共轭物是在聚合物或低聚物的聚合过程中形成的，其中药物被用作引发单体聚合的引发剂，这些单体形成聚合物和/或低聚物。更具体地说，药物共轭物是通过在适当的开环聚合催化剂和引发剂（药物）存在下的环开口聚合反应中形成的。该方法特别适用于形成聚合物/低聚物共轭物与含有一个或多个羟基或硫醇基团的药物和其他化学物质。
• MICROPARTICLES COMPRISING A SMALL HEAT-SHOCK PROTEIN
  申请人：Delta Crystallon B.V.

  公开号：EP2593088B1

  公开（公告）日：2015-01-07
• US9789195B2
  申请人：——

  公开号：US9789195B2

  公开（公告）日：2017-10-17
• [EN] SYSTEM FOR CONTROLLED DRUG DELIVERY COMPRISING BIODEGRADABLE POLYMER MICROPARTICLES<br/>[FR] SYSTÈME D'ADMINISTRATION CONTRÔLÉE DE MÉDICAMENT COMPORTANT DES MICROPARTICULES POLYMÈRES BIODÉGRADABLES
  申请人：UNIV UTRECHT HOLDING BV

  公开号：WO2010123349A1

  公开（公告）日：2010-10-28

  The present invention relates to systems for controlled release, such as controlled drug release. In particular, it relates to systems comprising biodegradable polymer microparticles based on hydrophilic polysters having pendant hydroxyl groups and obtainable from water-in-oil-in-water emulsions for controlled release of drugs and therapeutics, such as DNA, proteins, peptides. Further, the invention relates to a method to prepare such systems and the use of such systems.