4,4'-azobis(azidopropyl 4-cyanopentanoate) | 1280212-00-1

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4,4'-azobis(azidopropyl 4-cyanopentanoate)
• 英文别名: 4,4'-azobis(3-azidopropyl 4-cyanopentanoate)；3-Azidopropyl 4-[[5-(3-azidopropoxy)-2-cyano-5-oxopentan-2-yl]diazenyl]-4-cyanopentanoate；3-azidopropyl 4-[[5-(3-azidopropoxy)-2-cyano-5-oxopentan-2-yl]diazenyl]-4-cyanopentanoate
• CAS: 1280212-00-1
• 化学式: C₁₈H₂₆N₁₀O₄
• 分子量: 446.469
• InChiKey: KKKNAFUJKISVPU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  32
• 可旋转键数：
  18
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.78
• 拓扑面积：
  154
• 氢给体数：
  0
• 氢受体数：
  12

反应信息

• 作为产物：
  描述：

  3-叠氮基丙醇 、 4,4'-偶氮双(4-氰基戊酸) 在 4-二甲氨基吡啶 、 N,N'-二环己基碳二亚胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 以66%的产率得到4,4'-azobis(azidopropyl 4-cyanopentanoate)
  参考文献：
  名称：

  Polymeric drug delivery conjugates and methods of making and using thereof

  摘要：

  本文描述了一种可降解的药物传递共轭物，用于有效地将生物活性剂传递给受试者。药物传递共轭物包括水溶性高分子量线性可降解聚合物骨架，该骨架包括通过第一（主链）可切割连接子连接在一起的多个线性水溶性聚合物段，其中生物活性剂与至少一个水溶性聚合物段、至少一个可切割连接子或二者的组合共价结合。这些共轭物相对于先前技术的传递共轭物具有许多优点。本文还描述了制备和使用这些共轭物的方法。

  公开号：

  US09289510B2

文献信息

• Polymeric drug delivery conjugates and methods of making and using thereof
  申请人：Pan Huaizhong

  公开号：US09289510B2

  公开（公告）日：2016-03-22

  Described herein are biodegradable drug delivery conjugates for effectively delivering bioactive agents to a subject. The drug delivery conjugates comprise a water-soluble high molecular weight linear biodegradable polymer backbone comprising a plurality of linear water-soluble polymeric segments connected to one another by a first (main-chain) cleavable linker, wherein a bioactive agent is covalently bonded to at least one water-soluble polymeric segment, at least one cleavable linker, or a combination thereof. The conjugates possess numerous advantages over prior art delivery conjugates. Also described herein are methods for making and using the conjugates.

  本文描述了一种可降解的药物传递共轭物，用于有效地将生物活性剂传递给受试者。药物传递共轭物包括水溶性高分子量线性可降解聚合物骨架，该骨架包括通过第一（主链）可切割连接子连接在一起的多个线性水溶性聚合物段，其中生物活性剂与至少一个水溶性聚合物段、至少一个可切割连接子或二者的组合共价结合。这些共轭物相对于先前技术的传递共轭物具有许多优点。本文还描述了制备和使用这些共轭物的方法。
• Synthesis of biodegradable multiblock copolymers by click coupling of RAFT-generated heterotelechelic polyHPMA conjugates
  作者：Jiyuan Yang、Kui Luo、Huaizhong Pan、Pavla Kopečková、Jindřich Kopeček

  DOI：10.1016/j.reactfunctpolym.2010.10.005

  日期：2011.3

  A new strategy for the synthesis of biodegradable high molecular weight N-(2-hydroxypropyl)methacrylamide (HPMA)-based polymeric carriers has been designed. An enzyme-sensitive, alkyne-functionalized, chain transfer agent (CTA-GFLG-alkyne; N-alpha-(4-pentynoyl)-N-delta-(4-cyano-4-(phenylcarbonothioylthio)pentanoyl-glycylphenylalanylleucylglycyl)-lysine) was synthesized and used to mediate the reversible addition-fragmentation chain transfer (RAFT) polymerization and copolymerization of HPMA. Post-polymerization modification with 4,4'-azobis(azidopropyl 4-cyanopentanoate) resulted in the formation of heterotelechelic HPMA copolymers containing terminal alkyne and azide groups. Chain extension via click reaction resulted in high molecular weight multiblock copolymers. Upon exposure to papain, these copolymers degraded into the initial blocks. Similar results were obtained for copolymers of HPMA with N-methacryloylglycylphenylalanylleucylglycyl thiazolidine-2-thione and N-methacryloyl-glycylphenylalanylleucylglycyl-gemcitabine. The new synthetic method presented permits the synthesis of biocompatible, biodegradable high molecular weight HPMA copolymer-anticancer drug conjugates that possess long-circulation times and augmented accumulation in solid tumor tissue due to the enhanced permeability and retention effect. (C) 2010 Elsevier Ltd. All rights reserved.