2-azido-N,N-diethylethan-1-amine | 364589-22-0

• 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: 2-azido-N,N-diethylethan-1-amine
• 英文别名: (2-Azidoethyl)diethylamine；2-azido-N,N-diethylethanamine
• CAS: 364589-22-0
• 化学式: C₆H₁₄N₄
• mdl: MFCD14652234
• 分子量: 142.204
• InChiKey: OGUPQWIGBVGEOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  10
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  17.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-azido-N,N-diethylethan-1-amine 在 silver nitrate 作用下， 以 水 、 乙腈 为溶剂， 反应 48.0h， 生成
  参考文献：
  名称：

  叠氮化物官能化离子液体作为有吸引力的高氢燃料的合成与性能

  摘要：

  作为用于推进剂燃料的有毒和挥发性肼衍生物的可行替代品，高离子离子液体（ILs）具有广阔的前景，因此在过去十年中引起了越来越多的关注。为了利用叠氮基团的反应性和高能量密度，合成了一系列低成本且易于制备的叠氮化物官能化阳离子型离子液体，包括富含燃料的阴离子，例如硝酸根，双氰胺和硝基氰酰胺阴离子。和特点。与100％HNO 3接触时，所有基于双氰胺和硝基氰酰胺的离子液体均会自燃。这些高声区IL的密度在1.11–1.29 g cm -3的范围内变化，根据高斯09计算预测的密度比脉冲在289.9到344.9 s g cm -3之间。这两个关键物理特性的值比不对称二甲基肼（UDMH）的值高得多。在研究的化合物中，化合物IL-3b（即1-（2-叠氮基乙基）-1-甲基吡咯烷-1-基二氰胺）具有优异的综合性能，包括最低的粘度（30.9 M Pa s），宽的液体操作范围（ -70至205°C），最短的点火延迟时间（7

  DOI：

  10.1002/asia.201900364
• 作为产物：
  描述：

  N,N-二乙基氯乙胺 在 sodium azide 作用下， 以 水 为溶剂， 反应 15.0h， 生成 2-azido-N,N-diethylethan-1-amine
  参考文献：
  名称：

  Novel Thermoresponsive Polymers Tunable by pH

  摘要：

  Thermoresponsive polymers that are pH tunable were successfully synthesized by a combination of atom transfer radical polymerization (ATRP) and Cu(I) -catalyzed 1,3-dipolar cycloaddition of azide and alkynes (click chemistry). ATRP was employed to synthesize poly(2-hydroxyethyl methacrylate) (PHEMA), followed by introduction of alkyne groups using pentynoic acid, leading to PHEMA-alkyne. 2-Azidoethylamine, 2-azido-N,N-dimethylethylamine, and 2-azido-N,N-diethylethylamine were added to the PHEMA-alkyne backbone via click chemistry. Molecular weight, molecular weight distribution, and click reaction efficiency were determined by gel permeation chromatography (GPC) and H-1 NMR spectroscopy. The average molecular weight (M-n) of the resulting polymers ranged from 5.6 x 10(4) to 7.0 x 10(4) depending on the molecular architecture. The molecular weight distribution was low (M-n/M-n = 1.25-1.35). The transmission spectra of the 0.1 wt % aqueous solutions of the resulting polymers with different pH values at 650 nm were measured as a function of temperature. Results showed that the lower critical solution temperature (LCST) could be dramatically affected by solution pH. To give additional evidence for pH-responsive thermal transition, in-situ temperature-dependent H-1 NMR measurements in deuterated water (0.01 wt %) were conducted. The LCST values measured by in-situ H-1 NMR correlated well with those determined by turbidimetry.

  DOI：

  10.1021/ma102751p

文献信息

• Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors
  作者：Laurent Le Corre、Anne-Lise Girard、Johannes Aubertin、François Radvanyi、Catherine Benoist-Lasselin、Aurélie Jonquoy、Emilie Mugniery、Laurence Legeai-Mallet、Patricia Busca、Yves Le Merrer

  DOI：10.1039/b923882d

  日期：——

  A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55–89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.

  设计了一系列吡啶并[2,3-d]嘧啶类化合物作为FGFR3酪氨酸激酶的抑制剂，这些化合物可能与ATP结合位点的一个未开发区域发生相互作用。该化合物库通过高效的点击化学步骤构建，便于合成含有多种取代基的三唑类化合物。在合成的27个类似物中，超过一半的化合物在2微摩尔浓度下对体外FGFR3激酶活性表现出55-89%的抑制作用，其中一个化合物（19g）能够抑制转染HEK细胞中突变型FGFR3-K650M的自磷酸化。
• [EN] POLYNUCLEOTIDE CONSTRUCTS<br/>[FR] CONSTRUCTIONS POLYNUCLÉOTIDIQUES
  申请人：SOLSTICE BIOLOGICS LTD

  公开号：WO2018035380A1

  公开（公告）日：2018-02-22

  Disclosed are polynucleotide constructs having a strand linked to a moiety carrying one or more auxiliary moieties. Also disclosed are polynucleotide constructs interrupted with a sugar analogue, and polynucleotide constructs with stereochemical^ enriched phosphorothioates. The polynucleotide constructs may be provided as hybridized polynucleotide constructs. Also featured are methods of delivery a polynucleotide construct to a cell and methods of reducing the expression of a protein in a cell by contacting the cell with the disclosed polynucleotide construct or hybridized polynucleotide construct.

  揭示了具有与携带一个或多个辅助基团的基团相连的多核苷酸构造。还披露了被糖类似物中断的多核苷酸构造，以及具有立体化学富集的磷酸硫酸酯的多核苷酸构造。这些多核苷酸构造可以作为杂交多核苷酸构造提供。还包括将多核苷酸构造传递给细胞的方法，以及通过将细胞与披露的多核苷酸构造或杂交多核苷酸构造接触来减少细胞中蛋白质表达的方法。
• Side chain impacts on pH- and thermo-responsiveness of tertiary amine functionalized polypeptides
  作者：Chunsheng Xiao、Yilong Cheng、Yu Zhang、Jianxun Ding、Chaoliang He、Xiuli Zhuang、Xuesi Chen

  DOI：10.1002/pola.27048

  日期：2014.3.1

  The systemic investigation of the structural impacts of side chains on the pH‐ and thermo‐responsiveness of tertiary amine functionalized poly(l‐glutamate)s (TA‐PGs) was carried out. The TA‐PGs polymers were effectively synthesized by Cu(I)‐catalyzed azide‐alkyne cycloaddition click reaction of azido tertiary amines with poly(γ‐propargyl‐l‐glutamate) (PPLG). Turbimetric measurements were performed

  侧链上的pH的结构影响的系统调查和叔胺官能化聚（热响应性升-谷氨酸）S（TA-的PGs）中的溶液中进行。通过铜（I）催化的叠氮基叔胺与聚（γ-炔丙基-l-谷氨酸）（PPLG）的叠氮化物-炔烃环加成点击反应有效合成了TA-PGs聚合物。进行了比浊法测量，以表征TA-PG在水溶液中的pH和温度诱导的相变，这表明该性质对氮的结构依赖性取代基团和1,2,3-三唑环与侧链中叔胺基团之间的“连接基”。详细地讲，TA-PG的pH响应特性基本上由侧链中N-取代基团的疏水性决定，pH转变点（pH t）随着N-取代基团疏水性的增加而降低，而TA PG的温度响应性受N取代基或“连接基”的影响。具有中等N取代胺基（例如DEA，PR和PD）或支链“连接子”（例如iso-丙烯和2-甲基丙烯基）更可能表达因pH值变化而调整的LCST型相变。这项研究揭示的这些结构-属性关系将有助于开发TA-PG在智能药物输送系统中的应用。©2013
• Light and pH dual-sensitive biodegradable polymeric nanoparticles for controlled release of cargos
  作者：Yingchun Xia、Yunxiong Zeng、Ding Hu、Huihui Shen、Jianru Deng、Yanbing Lu、Xinnian Xia、Weijian Xu

  DOI：10.1002/pola.28528

  日期：2017.5.15

  HepG2 cells as well as SMCC‐7721 cells. More importantly, the prepared DOX‐loaded nanoparticles exhibited good anticancer ability for the two cells. The synthesized light and pH dual‐sensitive biodegradable polymeric nanoparticles were expected to be platforms for precisely controlled release of encapsulated molecules. © 2017 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2017, 55, 1773–1783

  在本文中，首次通过载有炔基侧基的两亲嵌段共聚物（乙二醇）之间的叠氮化物-炔炔点击化学反应，首次轻松制备了轻质和pH双敏感的嵌段共聚物PEG- b-聚（MPC-偶氮/ DEA） ）-聚（5-甲基-5-炔丙基氧羰基-1,3-二恶烷-2-一）（PEG- b-聚（MPC））和两种含叠氮化合物的偶氮苯衍生物（Azo-N 3）和2-叠氮基-1-乙基二乙胺（DEA-N 3）。聚合物纳米颗粒的光响应得益于偶氮苯链段，pH响应性归因于DEA部分。制备的共聚物可以自组装成球形胶束颗粒。通过紫外/可见光谱，动态光散射（DLS）和透射电子显微镜（TEM）研究了这些颗粒对双重刺激的形态变化。尼罗河红（NR）被用作探针，荧光光谱被用作在联合刺激下聚合物纳米颗粒中货物释放增强的证据。将抗癌药物DOX加载到纳米颗粒中，并且在双重刺激下可以从这些纳米颗粒中释放加载的DOX。MTT分析进一步证明了PEG- b -poly（MPC）和PEG-
• Synthesis and characterization of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for treatment of Alzheimer's disease
  作者：Jinggong Liu、Jun Qiu、Mingxue Wang、Ling Wang、Lijuan Su、Jinbo Gao、Qiong Gu、Jun Xu、Shi-Liang Huang、Lian-Quan Gu、Zhi-Shu Huang、Ding Li

  DOI：10.1016/j.bbagen.2014.05.005

  日期：2014.9

  Besides, compound 9g exhibited cholinesterase inhibitory activity, with its IC50 values of 0.86 μM and 0.51 μM for acetylcholinesterase and butyrylcholinesterase, respectively. In addition, compound 9g showed good anti-oxidation effect with oxygen radical absorbance capacity (ORAC) value of 2.29. Conclusions Compound 9g was found to be a potent multi-target-directed agent for Alzheimer's disease. General

  背景 阿尔茨海默氏病（AD）是一种进行性神经退行性脑部疾病，其特征在于痴呆，认知障碍和记忆力减退。不同的因素都与AD的发展，如增加的水平β淀粉样蛋白（β），乙酰胆碱，金属离子解除管制，超磷酸化的tau蛋白，和氧化应激。 方法 使用了下列方法：1的有机合成ħ -phenanthro [9,10- d ]咪唑衍生物，抑制自介导的和金属诱导A的β 1-42聚集，乙酰胆碱酯酶和丁酰胆碱酯酶抑制研究，抗氧化活性研究，CD，MTT分析，透射电子显微镜，斑点图分析，凝胶电泳，蛋白质印迹和分子对接研究。 结果 我们合成并表征了一种新型的1 H-菲[9,10- d ]咪唑衍生物作为AD治疗的多功能剂。我们的研究结果表明，大多数这些衍生物表现出强烈的一个β聚集抑制作用。化合物9克有74％A β 1-42聚集抑制在10μM浓度的效果，其IC 50为自感应甲μM6.5的值β 1-42聚集。该化合物还显示的金属介导的（铜很好的抑制作用2