4-[[(Tert-butyl)dimethylsiloxy]methyl]-2,6-dimethoxyphenyl 4-nitrophenyl carbonate | 1008144-99-7

• 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: 4-[[(Tert-butyl)dimethylsiloxy]methyl]-2,6-dimethoxyphenyl 4-nitrophenyl carbonate
• 英文别名: [4-[[tert-butyl(dimethyl)silyl]oxymethyl]-2,6-dimethoxyphenyl] (4-nitrophenyl) carbonate
• CAS: 1008144-99-7
• 化学式: C₂₂H₂₉NO₈Si
• 分子量: 463.56
• InChiKey: AFOOPWYFZFALJH-UHFFFAOYSA-N

物化性质

• 沸点：
  532.6±50.0 °C(Predicted)
• 密度：
  1.169±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.71
• 重原子数：
  32
• 可旋转键数：
  10
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  109
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  DL-氨基丙醇 、 4-[[(Tert-butyl)dimethylsiloxy]methyl]-2,6-dimethoxyphenyl 4-nitrophenyl carbonate 在 1-羟基苯并三唑 、 三乙胺 作用下， 以 四氢呋喃 为溶剂， 反应 1.08h， 以83%的产率得到[4-[[tert-butyl(dimethyl)silyl]oxymethyl]-2,6-dimethoxyphenyl] N-(2-hydroxypropyl)carbamate
  参考文献：
  名称：

  [EN] PROTEIN-POLYMER-DRUG CONJUGATES
  [FR] CONJUGUÉS MÉDICAMENT-POLYMÈRE-PROTÉINE

  摘要：

  本文描述了一种用于与基于蛋白质的识别分子（PBRM）共轭的聚合支架，以形成PBRM-聚合物-药物共轭物的聚合支架。该支架包括一个或多个末端马来酰亚胺基团。还公开了从该支架制备的PBRM-聚合物-药物共轭物。还描述了包括这些共轭物的组合物、它们的制备方法以及使用这些共轭物或它们的组合物治疗各种疾病的方法。

  公开号：

  WO2015054669A1
• 作为产物：
  描述：

  叔丁基二甲基氯硅烷 在 咪唑 、 4-二甲氨基吡啶 、 三乙胺 作用下， 以 四氢呋喃 、 N,N-二甲基乙酰胺 为溶剂， 反应 72.0h， 生成 4-[[(Tert-butyl)dimethylsiloxy]methyl]-2,6-dimethoxyphenyl 4-nitrophenyl carbonate
  参考文献：
  名称：

  [EN] PROTEIN-POLYMER-DRUG CONJUGATES
  [FR] CONJUGUÉS MÉDICAMENT-POLYMÈRE-PROTÉINE

  摘要：

  本文描述了一种用于与基于蛋白质的识别分子（PBRM）共轭的聚合支架，以形成PBRM-聚合物-药物共轭物的聚合支架。该支架包括一个或多个末端马来酰亚胺基团。还公开了从该支架制备的PBRM-聚合物-药物共轭物。还描述了包括这些共轭物的组合物、它们的制备方法以及使用这些共轭物或它们的组合物治疗各种疾病的方法。

  公开号：

  WO2015054669A1

文献信息

• PROTEIN-POLYMER-DRUG CONJUGATES
  申请人：MERSANA THERAPEUTICS, INC.

  公开号：US20150104407A1

  公开（公告）日：2015-04-16

  A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

  本文描述了一种用于与基于蛋白质的识别分子（PBRM）共轭的聚合支架，形成PBRM-聚合物-药物共轭物的聚合支架。该支架包括一个或多个末端马来酰亚胺基团。还披露了从该支架制备的PBRM-聚合物-药物共轭物。还描述了包含这些共轭物的组合物、它们的制备方法以及使用这些共轭物或它们的组合物治疗各种疾病的方法。
• Chemotherapeutic bone-targeted bisphosphonate prodrugs with hydrolytic mode of activation
  作者：Rotem Erez、Sharon Ebner、Bernard Attali、Doron Shabat

  DOI：10.1016/j.bmcl.2007.11.029

  日期：2008.1

  Osseous tissues are considered to be limited as therapeutic target sites due to their biological properties. We have designed and synthesized two kinds of hydrolytically activated chemotherapeutic prodrugs containing bisphosphonate, a bone-targeting moiety. The first can be conjugated to drug molecules with an available hydroxy group; the drug is attached to the bisphosphonate component through an ester-labile linkage. The second is for use with drug molecules with amine functional group. In this case, a self-immolative linker is used to attach the drug to the bisphosphonate component through a carbonate-labile linkage. The concept was demonstrated using the drugs camptothecin, which has a hydroxy functional group, and tryptophan, which is a model molecule for a drug with amine functionality. Both prodrugs showed significant binding capability to hydroxyapatite, the major component of bone, and were hydrolytically activated under physiological conditions. (c) 2007 Elsevier Ltd. All rights reserved.
• PROTEIN-POLYMER DRUG CONJUGATES
  申请人：Asana BioSciences, LLC

  公开号：US20240082417A1

  公开（公告）日：2024-03-14

  A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.