生物分子化学修饰用聚乙二醇衍生物的合成及应用

聚乙二醇衍生物由于具有良好的生物相容性和免疫原性而被广泛应用于生物分子的化学修饰。本文就聚乙二醇衍生物的合成以及在生物医学和生物技术领域中的应用进行综述，主要包括聚乙二醇衍生物的分类，常用的聚乙二醇衍生物的合成方法及其性能，以及聚乙二醇衍生物的应用等。     

杯芳烃的功能化修饰及其在分子识别中的应用

本文综述了近几年杯芳烃类人工受体在功能化修饰方面的研究进展, 主要讨论了新型功能化衍生物的合成及其超分子识别功能的应用。     

杯吡咯和杂杯吡咯的结构、合成与应用

杯吡咯以其特殊的结构和优异性能, 在主客体化学尤其是分子识别等方面的应用前景已备受关注, 合成新型功能化杯吡咯及其衍生物已成为超分子化学领域的研究热点之一. 近年来通过引入新型芳烃基体合成了结构和性能多样的杂杯吡咯. 主要介绍了功能化的杯吡咯和杂杯吡咯的结构、合成及其在分子识别等领域的应用.     

1－硫脲乙基－2－芳基－2－咪唑啉化合物的合成

１－硫脲乙基－２－芳基－２－咪唑啉化合物的合成刘运廷，章荣玲（山东工业大学数理系济南，２５００１４）关键词咪唑啉，硫脲基，芳基，合成咪唑啉衍生物由于具有缓蚀、杀菌、抗癌等活性而迅速发展￣［１，５］。作者曾研究过各种咪唑啉衍生物的合成￣［６］，系采用通...     

通过自由基加成环化反应制备香豆素衍生物的研究进展

香豆素衍生物是一类重要的杂环内酯化合物,广泛应用于有机合成、生物医药及荧光材料等领域。开发新型简单高效的功能化香豆素合成策略一直受到人们的关注,通过苯丙炔酸酯与各类自由基前驱体的直接自由基加成环化反应为香豆素衍生物的功能化修饰提供了一条简单、清洁、高效的合成路线。本文综述了近年来基于自由基加成环化历程制备各类功能化香豆素衍生物的新进展。     

芳氧乙酸－3，3－二甲基－2－羰基丁酯衍生物的合成与生物活性

芳氧乙酸－３，３－二甲基－２－羰基丁酯衍生物的合成与生物活性史延年，李士明，方建新（南开大学元素有机化学研究所，天津，３０００７１）关键词芳氧乙酸酯，合成，生物活性芳氧乙酸及其酯类衍生物具有良好的生物活性．作者曾以苯氧乙酸类化合物为母体，合成了一系列...     

聚苯乙烯担载聚氧乙烯咪唑啉类季铵盐的合成及催化性能

合成了共聚苯乙烯－二乙烯基苯担载四聚乙二醇苄基季铵盐及共聚苯乙烯－二乙烯基苯担载四聚乙二醇接２－（＋）－烷基－４,５－二氢咪唑啉类季铵盐,探讨了它们在ｎ－溴辛烷与碘化钾反应中的相转移催化活性。     

手性1—芳基—2,2—甲基—1,3—丙二醇

简要综述了手性１－芳基－２，２－二甲基－１，３－丙二醇及其衍生物在不对称合成中应用和反应，包括作为手性化学位移试剂、拆分试剂、辅助剂、配体和不对称合成中间体。     

N,N''''-二乙酸取代含噻吩环氮杂冠醚配体及其稀土配合物的合成与表征

N－功能化大环不仅环的空腔大小及环上配位原子种类对不同离子具有配位选择性，其功能化的官能团也会对大环配体的性质和选择性有很大影响，这类大环及其金属配合物，在药物试剂犤１犦，金属离子的分离与回收犤２犦，环境保护和新材料犤３犦等方面都有着广泛的应用前景。人们对N－功能化氮氧杂大环及其配合物研究较多犤４～６犦，而对N－功能化的氮氧硫杂大环研究并不多。为了进一步研究和开发这类大环配体及其性质，我们合成了一个新的功能化的大环配体（４，５：１４，１５二苯并－３，１６－二氧－２１－硫－７，１２－二氮双环犤１６…     

3－芳基－1（2H，4H）－吖啶酮衍生物的合成及其镇痛作用

３－芳基－１（２Ｈ，４Ｈ）－吖啶酮衍生物的合成及其镇痛作用韩光范，魏永慧，尹荣王进军姜贵吉（吉林医学院检验系吉林１３２００１）（吉林化工学院精细化工系吉林）（延边大学化学系延吉）关键词吖啶酮衍生物，合成，镇痛作用吖啶及吖啶酮类化合物具有抗疟、抗菌、抗...     

Environment-responsive polymers for coating of pharmaceutical nanocarriers

Polyethylene glycol derivatives, such as block copolymers of polyethylene glycol and diacyllipids (for example, phosphatidylethanolamine) are widely used for surface modification of various pharmaceutical carriers in order to impart them longevity in the body. To make polyethylene glycol detachable from the surface of pharmaceutical carrier and facilitate the interaction of the carrier with target cells when in pathological zone, we have prepared a set of polyethylene glycol-phosphatidylethanolamine block copolymers with the pH sensitive hydrazone bond between polyethylene glycol and phosphatidylethanolamine, which destabilizes at lowered pH values typical for tumors and inflammation zones. We have demonstrated that the stability of the hydrazone bond at normal physiological pH (7.4) as well as the rate of its hydrolysis at pH 6 and below strongly depend on the type of substitutions at this bond. Using aliphatic and aromatic aldehydes and ketones, polyethylene glycol-phosphatidylethanolamine block copolymers were prepared with different stabilities and degradation rates, which can be useful in constructing stimuli-sensitive pharmaceutical carriers. The text was sabmitted by the authors in English. This work was supported by the NIH grants RO1 HL55519 and RO1 CA121838 to V.P. Torchilin.     

Microwave-Assisted Synthesis of Quinoxalines in PEG-400

A rapid and efficient procedure for the synthesis of quinoxaline derivatives has been achieved by condensation of aryl-1,2-diamines with 1,2-dicarbonyl compounds catalyzed by polyethylene glycol under CEM-focused microwave-irradiation conditions.     

Sorption of adamantanes on polyethylene glycol-modified graphitized thermal soot

The thermodynamic characteristics of sorption of adamantane and its functional derivatives on graphitized thermal soot (GTS) modified with polyethylene glycol Carbowax 20M were determined by equilibrium gas chromatography. The resulting thermodynamic characteristics were analyzed and compared with the data measured for adamantanes on the surface of nonmodified GTS and polyethylene glycol deposited on an inert substrate. The solid carbon substrate was shown to affect the character of intermolecular interactions in the GTS-modifier system and the retention of framework compounds under the conditions of gas, liquid, and solid-state chromatography.     

Chromatographic behavior of some furan derivatives

Sulfides of the furan series and derivatives of furylthienylmethane are separated by gas-liquid chromatography. Heats of solution in polyethylene glycol adipate supported on alkali-treated diatomaceous brick are calculated. Interaction with the stationary phase is considered.     

A new application of derivatives of polychlorobiphenyls and polyethylene glycols

The reaction of congeners of Sovol technical mixture of polychlorobiphenyls with polyethylene glycols was studied. Mixtures of hydroxy and mono(polyethylene glycol)oxy derivatives were obtained. The mixtures synthesized, which are of low hazard, were used as additives to industrial oil to improve its tribological characteristics.

     

超高效凝胶色谱法测定聚乙二醇衍生物的分子量及其分布

采用超高效聚合物色谱(APC)技术,以单甲氧基聚乙二醇丙醛(m PEG_p ALD)为代表,测定了聚乙二醇衍生物的相对分子质量及其分布和杂质含量,优选了色谱柱和流动相,考察了样品质量浓度变化以及溶解时间等对测定结果的影响。优化后3根超高效凝胶色谱柱串联,在柱温40℃,流动相95%甲醇,流速0.5m L/min,示差折光检测条件下,对m PEG_p ALD的分子量及其分布进行测定,同时得到杂质的相对含量。结果测得m PEG_p ALD主成分的重均分子量(Mw)为19 444,分布指数(D)为1.01;杂质1的Mw为38 703,D为1.01,含量为1.31%;杂质2的Mw为61 036,D为1.00,含量为0.70%。与常规凝胶渗透色谱(GPC)相比,该方法分辨率高,分析速度快,能快速测定m PEG_p ALD的相对分子量及其分布,并能得到其纯度和杂质含量,为其工艺研发、质量控制提供了科学的依据,同时也可用于其它PEG衍生物的相对分子量及其分布和纯度的测定。     

Simultaneous separation of nonionic surfactants and polyethylene glycols by reversed phase high performance liquid chromatography

Summary The simultaneous separation of polyethylene glycol and its derivatives such as the lauryl alcohol and lauric acid ethoxylate oligomers was carried out by reversed phase high performance liquid chromatography. Branched fluorinated silica gel columns combined with evaporative light scattering detection were used for the characterization of nonionic surfactants. Lauryl alcohol ethoxylate oligomers were separated at 10°C with an isocratic eluent according to ethoxylate number and the retention time of the oligomers decreases with increasing ethoxylate number. The Van’t Hoff plots of retention factor of lauryl alcohol ethoxylate gave a complex cure, which is anomalous behavior for reversed phase high performance liquid chromatography. The anomalous Van’t Hoff plots were explained by a partial conformational change from polar to less polar conformers with increasing temperature. The most significant features for the analysis of the lauryl alcohol ethoxylate were the use of acetonitrile as mobile phase and operating temperature. The polyethylene glycol was separated according to ethoxylate number and the retention time of oligomers increased with increasing ethoxylate number. The Van’t Hoff plots of retention factor of polyethylene glycol had negative slopes. It was presumed that the polar conformation of the ethylene oxide chain decreased with increasing temperature. The lauryl alcohol ethoxylate and polyethylene glycol were separated simultaneously in gradient elution as a result of the conformational change of the ethylene oxide chain. As a practical example, lauric acid ethoxylate simultaneously separated into free polyethylene glycol, ethoxylate monolaurate and ethoxylate dilaurate in gradient elution.     

Synthesis of functionalised polyethylene glycol derivatives of naproxen for biomedical applications

The preparation of a series of mono-naproxen functionalised polyethylene glycol derivatives have been achieved. These compounds feature several different terminal functional groups, the identities of which have been chosen to facilitate conjugation of these hybrid molecules to nanomaterials.     

PEG-600: a facile and eco-friendly reaction medium for the synthesis of N-alkyl derivatives of indole-3-carboxyaldehyde

Abstract

A facile and eco-friendly methodology for the synthesis of N-alkyl/aralkyl derivatives of indole & indole-3-carboxyaldehydes mediated by polyethylene glycol as an efficient and green solvent is described.