TBDMS-六聚乙二醇-羟基 | 194281-47-5

• 物质功能分类: 催化剂及助剂 - 聚合物
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: TBDMS-六聚乙二醇-羟基
• 英文名称: 2-{2-[2-(2-{2-[2-(tert-butyldimethylsilanyloxy)ethoxy]ethoxy}ethoxy)ethoxy]ethoxy}ethanol
• 英文别名: 2,2,3,3-Tetramethyl-4,7,10,13,16,19-hexaoxa-3-silahenicosan-21-ol；2-[2-[2-[2-[2-[2-[tert-butyl(dimethyl)silyl]oxyethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethanol
• CAS: 194281-47-5
• 化学式: C₁₈H₄₀O₇Si
• 分子量: 396.597
• InChiKey: KRAXAZGPWJWDGC-UHFFFAOYSA-N

物化性质

• 沸点：
  430.9±40.0 °C(Predicted)
• 密度：
  0.998±0.06 g/cm3(Predicted)
• 保留指数：
  2432.3

计算性质

• 辛醇/水分配系数(LogP)：
  2.08
• 重原子数：
  26
• 可旋转键数：
  19
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  75.6
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  TBDMS-六聚乙二醇-羟基 在 甲基磺酰氯 、 三乙胺 、 sodium azide 作用下， 以 乙醇 为溶剂， 以71%的产率得到2-[2-[2-[2-[2-(2-Azidoethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy-tert-butyl-dimethylsilane
  参考文献：
  名称：

  Synthesis and analysis of polyethylene glycol linked P-glycoprotein-specific homodimers based on (−)-stipiamide

  摘要：

  A series of five homodimeric polyethylene glycol (PEG) linked homodimers based on the multidrug resistance reversal agent (-)-stipiamide were made and tested fur their ability to interact with P-glycoprotein, the protein responsible for multidrug resistance, using ATPase and photoaffinity displacement assays. Key reactions include a new alkoxide-mesylate displacement for the assembly of the PEG linkers and a double Sunogashira coupling reaction. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4039(01)00619-0
• 作为产物：
  描述：

  六甘醇 、 叔丁基二甲基氯硅烷 在 咪唑 作用下， 以 二氯甲烷 为溶剂， 反应 24.0h， 生成 TBDMS-六聚乙二醇-羟基
  参考文献：
  名称：

  用于固相有机合成的单分散低聚（氧乙烯）接枝聚苯乙烯树脂的合成和应用。

  摘要：

  在我们小组的初步研究中，我们发现聚（苯乙烯-氧乙烯）接枝共聚物（PS-PEG），例如TentaGel树脂，对于凝胶相（13）C NMR光谱是有利的。由于PS-PEG树脂提供的溶液状环境，可以实现附着部分的良好光谱质量，这对于非破坏性的树脂上分析非常有用。这种树脂的一般缺点是低载量和由PEG接头（> 50个单位）产生的光谱中的强信号。在这里，我们描述了一种用于固相有机合成（SPOS）的新型树脂的溶剂依赖性溶胀和反应动力学的表征，该树脂可通过凝胶相NMR进行精确监测而没有上述缺点。合成了一系列包含单分散PEG单元（n = 2-12）的聚苯乙烯-低聚（氧乙烯）接枝共聚物。在（13）C凝胶相光谱中观察到接头（PEG）长度和线宽之间存在很强的相关性，其中8个单元的PEG接枝链在反应性和凝胶相NMR监测方面与TentaGel相似，结果相似树脂。进行了多步树脂上反应序列以证明树脂在固相有机合成中的适用性。

  DOI：

  10.1021/co500028h

文献信息

• [EN] CONJUGATES COMPRISING PEPTIDE GROUPS AND METHODS RELATED THERETO<br/>[FR] CONJUGUÉS COMPRENANT DES GROUPES PEPTIDIQUES ET PROCÉDÉS ASSOCIÉS À CEUX-CI
  申请人：LEGOCHEM BIOSCIENCES INC

  公开号：WO2017089894A1

  公开（公告）日：2017-06-01

  In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.

  在某些方面，本发明涉及一种抗体药物偶联物，包括：抗体；连接体；以及至少两个活性剂。在优选的实施例中，连接体包括由多个氨基酸组成的肽序列，其中至少两个活性剂通过共价键与氨基酸的侧链连接。抗体药物偶联物可以包括自焚基团，优选地是两个自焚基团。连接体可以包括O-取代的肟，例如，其中肟的氧原子被取代以与活性剂形成共价键连接；肟的碳原子被取代以与抗体形成共价键连接。
• Ultra-Fast Dendritic Growth Based on the Grafting of Fullerene Hexa-Adduct Macromonomers onto a Fullerene Core
  作者：David Sigwalt、Rubén Caballero、Michel Holler、Jean-Marc Strub、Alain Van Dorsselaer、Jean-François Nierengarten

  DOI：10.1002/ejoc.201600439

  日期：2016.6

  A fullerene hexa-adduct building block bearing an azide functionality was prepared in six steps, and grafted onto a central fullerene core under copper-catalyzed azide–alkyne cycloaddition conditions. The resulting tridecafullerene derivative is a first generation dendrimer with 132 peripheral ethyl ester groups. This compound was characterized by different spectroscopic techniques (1H and 13C NMR

  带有叠氮化物官能团的富勒烯六加合物结构单元分六步制备，并在铜催化的叠氮化物-炔烃环加成条件下接枝到中心富勒烯核上。所得的十三富勒烯衍生物是具有 132 个外围乙酯基团的第一代树枝状聚合物。该化合物通过不同的光谱技术（1H 和 13C NMR、IR、UV/Vis）和 MALDI-TOF 质谱进行表征。尽管碎片化程度很高，但仍检测到分子离子峰，并且所有观察到的碎片均来自完全点击的衍生物。这表明从富勒烯六加合物大分子单体在单个树枝状生长步骤中构建树枝状大分子是生产单分散化合物的有效策略。
• Polyalkylene glycol derivatives of inhibitors of epidermal growth factor receptor tyrosine kinase
  申请人：Mishani Eyal

  公开号：US20080056990A1

  公开（公告）日：2008-03-06

  Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.

  本发明揭示了新型表皮生长因子受体酪氨酸激酶（EGFR-TK）抑制剂，包括同样的药物组合物及其在治疗EGFR-TK相关疾病或疾病中的应用。进一步揭示了新型放射性标记的EGFR-TK抑制剂，以及它们作为医学放射成像（如正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT））的生物标记物的应用，以及作为放射性药物用于放射治疗。所揭示的EGFR-TK抑制剂包括聚烷基醚基团和/或含羟基的基团，并具有改善的溶解性、生物稳定性和生物利用度。还揭示了制备所述EGFR-TK抑制剂和放射性标记同样的过程，例如一步放射合成。
• Synthetic Approaches to a Variety of Covalently Linked Porphyrin−Fullerene Hybrids
  作者：Shaun MacMahon、Robert Fong、Phil S. Baran、Igor Safonov、Stephen R. Wilson、David I. Schuster

  DOI：10.1021/jo010317x

  日期：2001.8.1

  There is substantial interest in dyads in which C-60 is covalently linked to electron donors, such as porphyrins, which absorb light strongly in the visible region. We present here the details of the syntheses of such compounds, which can be broadly organized into categories depending upon the nature of the linker joining the two chromophores. The structural aspects of intramolecular electronic interaction that we have sought to explore have dictated the synthetic strategies employed to generate these classes of molecules. Flexible glycol linkers were used to allow close approach between the fullerene and porphyrin, facilitating through-space interactions. These linkers also allowed studies of the effects of metal cation complexation. Naphthalene and alkyne linkers were used to examine the possible effects a conjugated or aromatic linker might have on photophysical properties. Finally, steroids were used as linkers in dyads expected to possess a large distance between the two chromophores, in which only through-bond interactions between the fullerene and porphyrin should be possible.
• [EN] CONJUGATES COMPRISING SELF-IMMOLATIVE GROUPS AND METHODS RELATED THERETO<br/>[FR] CONJUGUÉS COMPRENANT DES GROUPES AUTO-IMMOLABLES ET PROCÉDÉS ASSOCIÉS
  申请人：LEGOCHEM BIOSCIENCES INC

  公开号：WO2017089890A8

  公开（公告）日：2018-07-19