1-azido-10-bromodecane | 1325740-83-7

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 1-azido-10-bromodecane
• 英文别名: 1-Azido-10-bromo-decane
• CAS: 1325740-83-7
• 化学式: C₁₀H₂₀BrN₃
• 分子量: 262.193
• InChiKey: ZCTQLQPACJNJRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  14
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  14.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-azido-10-bromodecane 在 palladium 10% on activated carbon 、 氢气 、 potassium carbonate 、 N,N-二异丙基乙胺 、 三苯基膦 、 potassium iodide 作用下， 以 四氢呋喃 、 甲醇 、 溶剂黄146 、 异丙醇 、 正丁醇 为溶剂， 反应 113.0h， 生成 tert‐butyl N‐[({10‐[(10‐{[{[(tert‐butoxy)(hydroxy)methyl]imino}({[(tert‐butoxy)carbonyl]amino})methyl]amino}decyl)amino]decyl}amino)({[(tert‐butoxy)carbonyl]imino})methyl]‐N‐(cyclopropylmethyl)carbamate
  参考文献：
  名称：

  Alkyl-guanidine Compounds as Potent Broad-Spectrum Antibacterial Agents: Chemical Library Extension and Biological Characterization

  摘要：

  Nowadays, the increasing of multidrug-resistant pathogenic bacteria represents a serious threat to public health, and the lack of new antibiotics is becoming a global emergency. Therefore, research in antibacterial fields is urgently needed to expand the currently available arsenal of drugs. We have recently reported an alkyl-guanidine derivative (2), characterized by a symmetrical dimeric structure, as a good candidate for further developments, with a high antibacterial activity against both Gram-positive and Gram-negative strains. In this study, starting from its chemical scaffold, we synthesized a small library of analogues. Moreover, biological and in vitro pharmacokinetic characterizations were conducted on some selected derivatives, revealing notable properties: broad-spectrum profile, activity against resistant clinical isolates, and appreciable aqueous solubility. Interestingly, 2 seems neither to select for resistant strains nor to macroscopically alter the membranes, but further studies are required to determine the mode of action.

  DOI：

  10.1021/acs.jmedchem.8b00619
• 作为产物：
  描述：

  1,10-二溴癸烷 在 sodium azide 作用下， 以 二甲基亚砜 为溶剂， 反应 24.5h， 以94%的产率得到1-azido-10-bromodecane
  参考文献：
  名称：

  感知乙酰胆碱和抗胆碱酯酶化合物

  摘要：

  乙酰胆碱是关键的神经递质，抗胆碱酯酶是用作药物，杀虫剂和化学战剂的必需化合物。引入了一种基于半合成荧光的探针，可直接，实时检测乙酰胆碱和抗胆碱酯酶化合物。该探针具有良好的灵敏度，可调节的检测范围，并且可以选择性地靶向细胞表面，从而使其成为分析化学和定量生物学应用的有吸引力的工具。

  DOI：

  10.1002/anie.201307754

文献信息

• Bifunctional supramolecular prodrug vesicles constructed from a camptothecin derivative with a water-soluble pillar[5]arene for cancer diagnosis and therapy
  作者：Guangping Sun、Zhimei He、Min Hao、Zuqiang Xu、Xiao-Yu Hu、Jun-Jie Zhu、Leyong Wang

  DOI：10.1039/c9cc05859a

  日期：——

  Bifunctional supramolecular prodrug vesicles have been successfully constructed based on the complexation between a glutathione (GSH)-responsive prodrug guest molecule (DNS-CPT) and a water-soluble pillar[5]arene (WP5) for cancer diagnosis and therapy. Under the microenvironment of cancer cells with high GSH concentration, 7-ethyl-10-hydroxycamptothecin (SN-38) with strong yellow fluorescence can be

  基于谷胱甘肽（GSH）响应的前体药物客体分子（DNS-CPT）和水溶性支柱[5] arene（WP5）之间的复合作用，成功构建了双功能超分子前体囊泡，用于癌症的诊断和治疗。在高GSH浓度的癌细胞的微环境下，具有强黄色荧光的7-乙基-10-羟基喜树碱（SN-38）可以有效地从前药DNS-CPT中释放出来，用于药物定位和癌症治疗。
• Spirocentric Compounds and Polymers Thereof
  申请人：Georgia Tech Research Corporation

  公开号：US20190276454A1

  公开（公告）日：2019-09-12

  The present invention is directed to novel functionalized spirocentric compounds and polymers thereof that produce hyper-rigid cross-linked membranes.

  本发明涉及新型功能化螺环化合物及其聚合物，可产生超刚性交联膜。
• Silver-Catalyzed Decarboxylative Azidation of Aliphatic Carboxylic Acids
  作者：Yuchao Zhu、Xinyao Li、Xiaoyang Wang、Xiaoqiang Huang、Tao Shen、Yiqun Zhang、Xiang Sun、Miancheng Zou、Song Song、Ning Jiao

  DOI：10.1021/acs.orglett.5b02155

  日期：2015.10.2

  The catalytic decarboxylative nitrogenation of aliphatic carboxylic acids for the synthesis of alkyl azides is reported. A series of tertiary, secondary, and primary organoazides were prepared from easily available aliphatic carboxylic acids by using K2S2O8 as the oxidant and PhSO2N3 as the nitrogen source. The EPR experiment sufficiently proved that an alkyl radical process was generated in the process

  报道了用于烷基叠氮化物合成的脂肪族羧酸的催化脱羧氮化。通过使用K 2 S 2 O 8作为氧化剂和PhSO 2 N 3作为氮源，由易于获得的脂肪族羧酸制备出一系列的叔，仲和伯有机叠氮化物。EPR实验充分证明在该过程中产生了烷基自由基过程，DFT计算进一步支持SET过程，然后逐步进行S H 2反应以提供叠氮化物产物。
• Incorporation of a calixarene-based glucose functionalised bolaamphiphile into lipid bilayers for multivalent lectin recognition
  作者：S. Aleandri、A. Casnati、L. Fantuzzi、G. Mancini、G. Rispoli、F. Sansone

  DOI：10.1039/c3ob40732b

  日期：——

  glucosylated bolaamphiphile built on a calix[4]arene scaffold are described. The new glucocalixarene bolaamphiphile destabilizes bilayers of saturated lipids whereas it rigidifies those of unsaturated lipids, thus reducing leakage of calcein from the liposome internal aqueous compartment. Moreover, from fluorescence and turbidimetry experiments it was found that the glucose units of bolaamphiphile 1 functionalised

  描述了在杯[4]芳烃支架上构建的葡糖基化的两亲物的合成，表征和包含在脂质体中。新的葡糖杯芳烃硼两亲物使饱和脂质的双层不稳定，而使不饱和脂质的双层僵化，从而减少了脂质的渗漏。钙黄绿素从脂质体的内部水室。此外，从荧光和比浊法实验中发现，Boampamphiphil 1官能化脂质体的葡萄糖单元可与四聚体葡萄糖结合蛋白伴刀豆球蛋白A进行特定的多价相互作用。因此，这些结果代表了一种利用糖功能化脂质体，利用多价糖基化配体的新颖策略。用于制备可能靶向特定凝集素的药物输送系统。
• Pseudomonas aeruginosa inhibitor compounds
  申请人：Centre National de la Recherche Scientifique (CNRS)

  公开号：US10908153B2

  公开（公告）日：2021-02-02

  The invention relates to a method of identifying molecules which inhibit the virulence machinery of Pseudomonas aeruginosa, to a device for identifying a molecule which inhibits the virulence machinery of Pseudomonas aeruginosa, to novel compounds which inhibit the virulence machinery of Pseudomonas aeruginosa, to compounds for use for preventing and/or treating a pathogenic infection caused by Pseudomonas aeruginosa and also to pharmaceutical compositions for preventing and/or treating a pathogenic infection caused by Pseudomonas aeruginosa.

  本发明涉及一种鉴定抑制铜绿假单胞菌毒力机制的分子的方法，涉及一种鉴定抑制铜绿假单胞菌毒力机制的分子的装置，涉及抑制铜绿假单胞菌毒力机制的新型化合物，涉及用于预防和/或治疗铜绿假单胞菌引起的病原体感染的化合物，还涉及用于预防和/或治疗铜绿假单胞菌引起的病原体感染的药物组合物。