tert-butyl bis(2-(2-(tosyloxy)ethoxy)ethyl)carbamate | 1042743-76-9

• 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: tert-butyl bis(2-(2-(tosyloxy)ethoxy)ethyl)carbamate
• 英文别名: 2-[2-[2-[2-(4-Methylphenyl)sulfonyloxyethoxy]ethyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]ethoxy]ethyl 4-methylbenzenesulfonate；2-[2-[2-[2-(4-methylphenyl)sulfonyloxyethoxy]ethyl-[(2-methylpropan-2-yl)oxycarbonyl]amino]ethoxy]ethyl 4-methylbenzenesulfonate
• CAS: 1042743-76-9
• 化学式: C₂₇H₃₉NO₁₀S₂
• 分子量: 601.739
• InChiKey: SFYQUFNMVZVEKM-UHFFFAOYSA-N

物化性质

• 沸点：
  702.8±60.0 °C(Predicted)
• 密度：
  1.242±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  40
• 可旋转键数：
  18
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.52
• 拓扑面积：
  152
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  tert-butyl bis(2-(2-(tosyloxy)ethoxy)ethyl)carbamate 在 potassium carbonate 、 三氟乙酸 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 10.0h， 生成 2-(4-(2-(2-((2-(2-hydroxyethoxy)ethyl)(pyridin-4-ylmethyl)amino)ethoxy)ethoxy)phenyl)-4H-chromen-4-one
  参考文献：
  名称：

  SYNTHESIS AND USE OF AMINE-CONTAINING FLAVONOIDS AS POTENT ANTI-LEISHMANIAL AGENTS

  摘要：

  本发明涉及一种新型的含胺类黄酮类化合物系列和含有这些化合物的组合物，以及它们的合成和使用。该发明还涉及治疗和预防疾病的方法，特别是包括利什曼病在内的寄生虫感染，其中包括给予这些化合物。

  公开号：

  US20150239870A1

文献信息

• [EN] FLAVONOID DIMERS AND THEIR USE<br/>[FR] DIMÈRES FLAVONOÏDES ET LEURS APPLICATIONS
  申请人：UNIV MCGILL

  公开号：WO2011137516A1

  公开（公告）日：2011-11-10

  This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.

  这项发明涉及到公式为黄酮素-连接子-Y-连接子-黄酮素的双黄酮类化合物，它们的合成以及在化疗和原虫感染中抑制多药耐药性的用途。
• Amine Linked Flavonoid Dimers as Modulators for P-Glycoprotein-Based Multidrug Resistance: Structure–Activity Relationship and Mechanism of Modulation
  作者：Kin-Fai Chan、Iris L. K. Wong、Jason W. Y. Kan、Clare S. W. Yan、Larry M. C. Chow、Tak Hang Chan

  DOI：10.1021/jm201121b

  日期：2012.3.8

  Here we report a great improvement in reversal potency of cancer drug resistance when flavonoid dimers possess a functionally substituted aminopolyethylene glycol linker. The most potent compound, 18, contains a N-benzyl group at the linker. It has many advantages including (1) high potencies in reversing P-glycoprotein (P-gp) mediated resistance in LCC6MDR cells to various anticancer drugs with EC50 in the nanomolar range, (2) low toxicity and high therapeutic index, and (3) preferential inhibition of P-gp over multidrug resistance protein 1 and breast cancer resistance protein. Compound 18 stimulates P-gp-ATPase activity by 2.7-fold and mediates a dose-dependent inhibition of doxorubicin (DOX) transport activity. Lineweaver-Burk and Dixon plots suggest that 18 is a competitive inhibitor to DOX in binding to P-gp with a K-i of 0.28-0.34 mu M and a Hill coefficient of 1.17. Moreover, the LCC6MDR cell displays about 2.1-fold lower intracellular accumulation of 18 compared to the wild type, suggesting that 18 is a P-gp substrate as well.
• FLAVONOID DIMERS AND THEIR USE
  申请人：Chan Tak-Hang

  公开号：US20130045935A1

  公开（公告）日：2013-02-21

  This invention relates to bis-flavonoid compounds of formula Flavonoid-Linker-Y-Linker-Flavonoid, their synthesis and use for inhibiting multidrug resistance in chemotherapy and protozoan infection.
• TETRAMALEIMIDE LINKERS AND USE THEREOF
  申请人：NewBio Therapeutics, Inc.

  公开号：US20210128668A1

  公开（公告）日：2021-05-06

  The present invention is directed to tetramaleimide linkers and use thereof, more specifically to the compounds represented by formula I and their use in the preparation of antibody-drug conjugates (ADCs). The ADCs obtained from the tetramaleimide linkers have high homogeneity and stability, and could be used effectively for the treatment of various diseases including tumors. The definition of the groups in formula I is the same as that in the description.
• US8980848B2
  申请人：——

  公开号：US8980848B2

  公开（公告）日：2015-03-17