CAS: 14691-88-4; 4-Amino-2,2,6,6-Tetramethylpiperidine 1-Oxyl

该化合物是一种稳定的氮氧化基,其独特的结构特征是含有四组甲基和氨基组的管状环,该化合物因其具有未受保护的电子的存在而具有的磁性,有助于其稳定性和反应性,因此值得注意.TEMPOL经常用于各种应用,包括作为电子对磁共振光谱学以及生物和制药研究的旋转标签,因为它具有抗氧化特性.它可以对自由基进行搜索,使其成为与氧化性压力和细胞保护有关的研究的一个对象.此外,对TEPOL在包括心血管疾病和...

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14691-89-5 2564-83-2 7031-93-8

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4-AMINO-2,2,6,6-TETRAMETHYLPIPERIDINE 4-oxo-2,2,6,6-tetramethylpiperidin-oxyl 4-azido-2,2,6,6-tetramethyl-1-piperidinyloxy radical N,N:N',N'-di-1,2-ethanediyl-N''-(1-oxy-2,2,6,6-tetramethyl-4-piperidyl)phosphorothioic triamide 2,2,6,6-tetramethylpiperidine-1-oxyl-4-succinamic acid bis(p-nitrophenyl) 1-oxy-2,2,6,6-tetramethyl-4-piperidinyl phosphoramidate triethylamine hydr°Chloride

合成工艺路线路线简述

    四甲基哌啶酮置于sodium Tungstate (Vi) Dihydrate,乙二胺四乙酸,Ammonium Acetate,双氧水,Sodium Cyanoborohydride体系中,用 甲醇,水 用作溶剂,化学反应 96.0H,反应生成4-氨基-Tempo
    参考文献:带有自旋标记抑制剂dcc和archazolid的v‐atpase的epr研究:质子易位亚基c的相互作用动力学
    标题:带有自旋标记抑制剂dcc和archazolid的v‐atpase的epr研究:质子易位亚基c的相互作用动力学
    摘要:液泡型h +-Atpases(v-Atpases)作为高度有希望的抗癌药物靶标最近受到关注,因此详细的结构分析和抑制剂相互作用的研究是非常重要的研究目标.通过两种新颖的方法共价结合(2,2,6,6-四甲基哌啶-1)来自旋分离烟草酵母(saccharomyces Cerevisiae)液泡中的烟草天蛾manduca Sexta的v-Atpase全酶和v-Atpase的自旋标记.N,N'的‐yl)氧基(tempo)衍生物-二环己基碳二亚胺(dcc)与活性位点中的必需谷氨酸残基以及强效抑制剂archazolid(一种来自粘菌的天然产物)的自由基类似物的非共价相互作用.通过电子顺磁共振(epr)光谱研究和双电子-电子共振(deer)测量对这两种配合物进行了详细评估,从而揭示了对抑制剂结合模式,动力学和化学计量以及对中央功能亚基c的了解.这些具有医学重要性的异质多聚体质子转运蛋白.这项研究还证明了
    Doi:10.1002/cmdc.201500500

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    专利信息


    专利号:WO-2013182636-A1
    优先权日:2012-06-07
    标 题 :Synthesis of a viral protease inhibitor
    发明人:ALLEGRINI PIETRO; BRUNOLDI ENRICO; ATTOLINO EMANUELE
    权利人:DIPHARMA FRANCIS SRL
    摘要:Disclosed is a process for the preparation of telaprevir of formula (I) or a salt thereof, comprising the oxidation reaction of a compound of formula (II) or a salt thereof, (II) wherein said oxidation is conducted in a solvent in the presence of a supported oxidising agent.

    专利号:US-7205385-B2
    优先权日:2004-11-12
    标 题:Polymerization method for the synthesis of polypeptide imaging agents
    发明人:GRIMMOND BRIAN JAMES; MOASSER BAHRAM; AMARATUNGA MOHAN MARK
    权利人:GEN ELECTRIC
    摘要:A method for synthesizing extended poly(amino acids) conjugated to imaging agents, such as DTPA, is disclosed. The amino acid is initially conjugated to the imaging agent at the monomer stage, followed by formation of the corresponding N-carboxyanhydride. The method utilizes catalyzed ring opening polymerization of the N-carboxyanhydride of the amino acid-imaging agent monomer allowing the formation of a poly(amino acid) backbone having 100% imaging agent conjugation if desired. However, the present method also permits the degree of conjugation to be controlled by copolymerizing the N-carboxyanhydride of the amino acid-imaging agent monomer with one or more unconjugated monomers, i.e. N-carboxyanhydrides of the same or of other amino acids. Various imaging agents may be employed, and new hybrid random, block, and mixed copolymers may be prepared.

    专利号:WO-2024256666-A1
    优先权日:2023-06-16
    标 题:Production of synthesis gas by partial oxidation of a hydrocarbon stream containing plastic liquefaction oil
    发明人:ADAM CINDY; CHOFFAT ALEXANDRINE; MINOUX DELPHINE; VAN LOOK EMMANUEL; BRETON CHRISTOPHE
    权利人:TOTALENERGIES ONETECH
    摘要:The invention relates to a process for the production of synthesis gas by partial oxidation from a hydrocarbon stream containing plastic liquefaction oil, comprising: a) providing a composition stabilized against premature polymerization comprising: 1) a hydrocarbon stream containing at least 2 wt% of plastic liquefaction oil which is containing contaminants, the remaining part of said hydrocarbon stream being a diluent, 2) at least one additive capable to reduce gums formation or buildup, 3) optionally at least one additive which is a dispersant agent, b) an optional purification step to trap silicon and/or metals and/or phosphorous and/or halogenates over at least one trap to obtain a purified composition, c) gasifying by partial oxidation the stabilized composition provided in step (a), or the purified composition provided in step (b), in a partial oxidation gasification unit to produce synthesis gas comprising at least dihydrogen, carbon monoxide, and carbon dioxide.

    专利号:US-2002055124-A1
    优先权日:1998-09-23
    标题:Soluble support for organic synthesis
    发明人:JANDA KIM D; GRAVERT DENNIS J
    权利人:SCRIPPS RESEARCH INST
    摘要:Polymer supports for liquid-phase organic synthesis (LPOS) are employed in a process for transferring a chemical intermediate between immiscilbe solvents. These compounds are produced with an expanded range of solubility range in a variety of solvent systems. A sequence of normal and “livingâ€? free radical polymerizations are employed to generate a library of block copolymers possessing either block or graft architecture with initiators 100, 200 and 3 - 4 and a diverse set of vinyl monomers 5 - 9 . Novel bifunctional initiators are employed that have functional groups that independently produce free radical polymerizations to produce the block copolymers. Preferred functional groups include diazene (—Nâ•?N—) and 2,2,6,6-tetramethylpiperidinyl-1-oxy (TEMPO) moieties tethered by ester or ether linkages.

    专利号:WO-2020120582-A1
    优先权日:2018-12-11
    标题:Chromenic phytocannabinoids, their synthesis and use in treatment or prevention of disease
    发明人:MUÑOZ BLANCO EDUARDO; APPENDINO GIOVANNI; UNCITI BROCETA JUAN DIEGO
    权利人:EMERALD HEALTH BIOTECHNOLOGY ESPANA S L U
    摘要:The present invention relates to a compound of the formula (I) or a solvate or co-crystal thereof (I) wherein: - R is selected from the group consisting of: a C1-C6 alkyl, a C2-C8 alkenyl moiety, a C4-C12 dienyl or a C6-C18 trienyl moiety; - R1 is a C1-C6 alkyl moiety; - R2 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R3 is selected from the group consisting of: H and a C1-C6 alkyl moiety; - R4 is selected from the group consisting of: H, a C1-C6 alkyl moiety and a benzyl moiety. The present invention also relates to a process for producing said compound of the formula (I), or a solvate or co-crystal thereof, as well as a pharmaceutical composition comprising said compound of the formula (I), or a solvate or co-crystal thereof and at least one excipient. The present invention also relates to a compound of the formula (I), or a solvate or co-crystal thereof, for use in the treatment or prevention of a disease or condition.

    专利号:US-2007160574-A1
    优先权日:2000-04-12
    标题 :Design of CXC chemokine analogs for the treatment of human diseases
    发明人:MERZOUK AHMED; SALARI HASSAN
    权利人:MERZOUK AHMED; SALARI HASSAN
    摘要:The present invention generally relates to the design, preparation, derivation, and use of mimetics of CXC chemokines (CXCL1-CXCL17) in the prevention, treatment, and ameliorization of a wide variety of diseases and disorders. Generally speaking, this invention is directed to the design, synthesis, and use of chemokine analogs which bind to CXC chemokine receptors CXCR1-CXCR7, such that the analogs can be designed to affect the activity of the receptor, either as an agonist or an antagonist. The analogs can be useful for treating a wide variety of diseases and disorders, and can also serve as an adjunct to the treatment of a variety of diseases and disorders.
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    主要参考文献

    [参考文献]: Gabriela Ionita, Et Al. Ion Exchange In Alginate Gels--Dynamic Behaviour Revealed By Electron Paramagnetic Resonance. Soft Matter. 2015 Dec 14;11(46):8968-74.
    [参考文献]: J Czepas, Et Al. Different Effectiveness Of Piperidine Nitroxides Against Oxidative Stress Induced By Doxorubicin And Hydrogen Peroxide. Cell Biol Toxicol. 2008 Jan;24(1):101-12.
    [参考文献]: Jesus Vazquez, Et Al. Development Of Molecular Probes For Second-Site Screening And Design Of Protein Tyrosine Phosphatase Inhibitors. J Med Chem. 2007 May 3;50(9):2137-43.
    [参考文献]: Jianhua Zhang, Et Al. Synthesis Of Nanogels Via Cell Membrane-Templated Polymerization. Small. 2015 Sep 9;11(34):4309-13.
    [参考文献]: Keren Turjeman, Et Al. Nano-Drugs Based On Nano Sterically Stabilized Liposomes For The Treatment Of Inflammatory Neurodegenerative Diseases. Plos One. 2015 Jul 6;10(7):E0130442.

    合成参考文献


    摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2013) 2, 314.
    摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2013) 2, 292.
    参考文献:10.1080/10611860600648429
    摘要:Jubeh TT, Nadler-Milbauer M, Barenholz Y, Rubinstein A. Local treatment of experimental colitis in the rat by negatively charged liposomes of catalase, TMN and SOD. J Drug Target. 2006 Apr;14(3):155–63. doi: 10.1080/10611860600648429.
    摘要:Keana JF, Pou S. Nitroxide-doped liposomes containing entrapped oxidant: an approach to the "reduction problem" of nitroxides as MRI contrast agents. Physiol Chem Phys Med NMR. 1985;17(2):235–40.
    参考文献:10.1016/0167-4889(86)90041-8
    摘要:Herrmann A, Müller P. Correlation of the internal microviscosity of human erythrocytes to the cell volume and the viscosity of hemoglobin solutions. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research. 1986 Jan;885(1):80–7. doi: 10.1016/0167-4889(86)90041-8.
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