维生素B12环B酰亚胺前体及琥珀胺类药物不对称合成的研究

从γ－丁内酯合成了维生素Ｂ１２环Ｂ酰亚胺前体及琥珀酰胺类药物的３个衍生物,进行了其中不对称季碳的构筑,改进了ＴｉＣｌ３还原硝基乙烯类化合物的反应,同时发现了一个简便合成乙琥酰胺环的新方法。     

四种选择性β2受体药物在不同酰胺型固定相上的拆分

比较了四种选择性β2受体手性药物氯丙那林、沙丁胺醇、克伦特罗以及丙卡特罗在Whelk-O1、DNB-PG、DNB-Leucine和SH-1等四种刷型酰胺手性固定相上的对映体直接拆分行为,考察了被分离化合物分子结构、固定相分子结构等因素对对映体分离选择性的影响,对药物与固定相分子的手性识别机理进行了初步探讨,给出了药物分...     

液晶性芳香酰胺化合物的合成

合成了一系列炖粹以酰胺基为中心桥键的刚性芳香酰胺小分子化合物，并对其作了表征，发现其中有些化合物具有液晶性。酰胺键之间能形成很强的分子间氢键，使芳香酰胺小分子化合物的熔点很高，难于形成液成液晶态。研究发现，如果在这类化合物的中心苯环上引入合适的取代基以减弱分子间氢键，同时引入合适的末端基时，则可使芳香酰胺化合物生成液晶相的能力增强。     

热致液晶性聚酯酰胺的研究进展

热致液晶性聚酯酰胺由于其独特的化学结构，形成了一新的液晶聚合物体系，本文就类热致性晶聚合物体系的研究进展作进行了述评。     

具有生理活性的甾体酰胺类化合物

在甾体的甾核或支链上引入不同的官能团后可得到不同生理活性的化合物,它们有可能会成为人类治疗不同疾病的药物,因此甾体药物除了作为传统激素类药物使用外,在抗肿瘤药物、抗炎药物中的应用也成为甾体的重要研究内容之一。含有酰胺官能团的甾体化合物具有很好的生物活性。本文按照酰胺基团在甾体酰胺化合物中的位置进行分类,同时结合本课题组在甾体酰胺化合物的合成和生理活性研究方面所取得的一些成果,概述了近几年来新合成及发现的甾体酰胺类化合物及其衍生物的生理活性及研究进展,包括作为抗肿瘤药物的甾体酰胺化合物的设计、筛选、对5α-还原酶的抑制作用、抑制肿瘤细胞生长增殖活性及抗菌作用,并对此方面的发展趋势、应用前景作了展望。     

酶催化合成酰胺类化合物的研究进展

酰胺官能团具有重要的药理作用，是许多生物活性物质的关键结构单元。据报道，超过25%的已知药物中含有酰胺键结构。研究与发展酰胺类化合物的高效合成方法始终是制药行业的重要任务之一。近年来，生物催化技术的发展为酰胺键的构建提供了一种较为经济绿色的合成方法，丰富了酰胺类化合物的合成策略。本文综述了生物酶催化合成酰胺类化合物的相关研究进展。      

酰胺类萃取剂萃取分离铕的研究进展

酰胺类萃取剂容易合成,热稳定性好,能完全燃烧,对环境友好等一系列优点,已广泛的用来从核燃料的后循环中萃取分离镧系元素和锕系元素。论述了使用不同类型的酰胺类萃取剂萃取及其分离铕的研究,重点讨论了丙二酰胺类和丁二酰胺萃取剂、酰胺莢醚类萃取剂、吡啶二甲酰胺类萃取剂、乙酰胺基胺类萃取剂萃取分离铕的最新研究成果,同时对这几类催化剂萃取铕的萃取效果进行了比较和讨论。     

壳聚糖/生发药物缓释膜的制备及性能

报道了壳聚糖生发药物缓释膜的制备、性能。确定了壳聚糖溶液成膜的最佳条件 ,用 3 5× 1 0 -5mol L壳聚糖溶液、0 2mol L的乙醇和少量甘油 ,制备的壳聚糖膜抗拉强度为 5 3 5 0 8N m。用UV分光光度法测定了生发药物缓释膜在水中的释放速率 ,对膜的缓释机理进行了初步探讨     

芳基脂肪基代异方酰胺的合成

实现了对称芳基代异方酰胺与一些脂肪胺的选择性部分酰胺交换反应，该反应提供了制备既含基又含脂肪基的不对称取代异方酰胺的一种非常有效的通用方法。     

脂肪族酰胺二元醇的合成与表征

以ＤＬ－乳酸、ε己内酯及乙二胺和己二胺为原料合成了四种结构的脂肪族酰胺二元醇，并用ＩＲ，＾１ＨＮＭＲ，ＤＳＣ对酰胺二元醇的结构进行了表征。     

Alkaline degradation behavior of polyesteramide fibers: surface erosion

In this work, a new kind of aliphatic polyesteramide (PEA) copolymer based on -caprolactone and 6-aminocaproic acid was synthesized by the melt polycondensation method. Biodegradable PEA fibers were processed by the melt-spinning method. ¹H-NMR, FTIR, SEM, and tensile testing were used to characterize the degradation of PEA fibers in concentrated alkaline solution. The PEA fiber undergoes surface erosion in such concentrated alkaline solutions.     

由对苯二甲酰胺二醇合成聚酯酰胺及其扩链反应的研究

以N,N′-二(2-羟乙基)对苯二甲酰胺与己二酸及丁二醇缩聚,合成了同时带有端羧基与端羟基的聚酯酰胺预聚体,研究了不同扩链剂的扩链反应,获得了特性黏度达1.05 dL/g的聚酯酰胺.对预聚体及扩链后聚合物进行了红外与核磁表征,研究了聚合物的结构,并对聚合物进行了DSC与TG分析.     

Preparation of biodegradable polyesteramide microspheres

Biodegradable polyesteramide copolymer P(CL/AU) based on -caprolactone and 11-aminoundecanoic acid was synthesized by the melt polycondensation method. Polyesteramide (PEA) microspheres were prepared by a simple O/W emulsion solvent evaporation method. The effects of variations in preparation parameters (such as emulsifier concentration, polymer concentration, polymer solution adding rate, stirring rate, and whether vacuum was applied) were studied in detail. The obtained microsphere morphologies were observed using an optical microscope and via scanning electron microscopy (SEM). The particle size distribution was determined using a Malvern laser particle sizer. When the PEA microspheres were incubated in PBS saline, the particle size increased at first, and then decreased after a longer time period; the theory that this behavior was due to degradation of the microspheres was confirmed by SEM.     

聚酯酰胺的合成及表征

用两种方法合成了聚酯酰胺（ＰＥＡ）共聚物．一种是两步法，即先合成对苯二甲酸乙醇酰胺（ＢＡＥＴ）单体，然后与对苯二甲酸乙二酯（ＢＨＥＴ）共缩聚；另一种是一步法．即在酯交换反应中直接添加乙醇胺（ＥＡ）．两种方法制得的聚酯酰胺（ＰＥＡ）共聚物测试证明了为产物，并分析了合成中的化学反应．     

聚酯酰胺的合成及表征

 用两种方法合成了聚酯酰胺（ＰＥＡ）共聚物．一种是两步法，即先合成对苯二甲酸乙醇酰胺（ＢＡＥＴ）单体，然后与对苯二甲酸乙二酯（ＢＨＥＴ）共缩聚；另一种是一步法．即在酯交换反应中直接添加乙醇胺（ＥＡ）．两种方法制得的聚酯酰胺（ＰＥＡ）共聚物测试证明了为产物，并分析了合成中的化学反应．     

Biodegradable Multiphase Systems Based on Plasticized Starch: A Review

Abstract

The aim of this review is to show the relationships between the structure, the process, and the properties of biodegradable multiphase systems based on plasticized starch (PLS), the so‐called “thermoplastic starch.” These mutiphase materials are obtained when associating association between plasticized starches and other biodegradable materials, such as biodegradable polyesters [polycaprolactone (PCL), polyhydroxyalkanoates (PHAs), polylactic acid (PLA), polyesteramide (PEA), aliphatic, and aromatic copolyesters], or agro‐materials (ligno‐cellulosic fiber, lignin etc.). Depending on materials (soft, rigid) and the plastic processing system used, various structures (blends, composites, multilayers) can be obtained. The compatibility problematic between these hetero‐materials is analyzed. These starchy products show some interesting properties and have some applications in different fields: packaging, sports, catering, agriculture and gardening, or hygiene.     

Capillary and slit-die flow of two liquid-crystalline polymers. The effect of pressure on viscosity

Viscosity measurements on two commercial thermotropic liquid crystalline polymers (LCPs) (a copolyester and a polyesteramide) were performed using both capillary and slit die methods. The results are in agreement with those presented in the literature for the same LCPs, when the measurements are carried out with a L/D = 30 die; these results are affected more by Bagley corrections for the polyesteramide than for the copolyester. For both LCPs, viscosities measured in the slit die are lower than those obtained by capillary rheometry. Nevertheless, the difference is much bigger in the case of the polyesteramide, for which a reduction by a factor of 3 is observed. This is not due to the preshear or thermal history, since the same piston-barrel system and thermal treatment were applied in both types of measurements. Depending on the polymer sample and temperature, concave and convex curvatures were observed in the pressure profiles during the slit flow. From these curvatures, the pressure coefficient α of viscosity was evaluated. However, in the case of the polyesteramide the convex curvature leads to a negative coefficient (the viscosity decreases with pressure, instead of increasing). This result may be explained by envisaging a change in the structure of the melt along the slit length. © 1993 John Wiley & Sons, Inc.     

Novel Biodegradable and pH‐Sensitive Poly(ester amide) Microspheres for Oral Insulin Delivery

Biodegradable and pH‐sensitive PEAs based on dual amino acids are designed, synthesized, and characterized. Insulin can be loaded into the PEA microspheres by a solid‐in‐oil‐in‐oil technique with high encapsulation efficiency. The feasibility of PEA microspheres as oral insulin delivery carriers is evaluated in vitro and in vivo. The hydrophobic leucine groups on PEA seem to play an important role in the pH‐dependent release mechanism and cytotoxicity of PEA microspheres. Oral administration of insulin‐loaded PEA microspheres to streptozotocin‐induced diabetic rats at 60 IU kg^?1 is able to reduce fasting plasma glucose levels to 49.4%. These results indicate that PEA microspheres are potential new vehicles for insulin oral delivery.

     

Poly(ether tert‐amine): A novel family of multiresponsive polymer

A novel multiresponsive poly(ether tert‐amine) (PEA) was synthesized by nucleophilic addition/ring‐opening reaction of commercial poly(ethylene oxide) (PEO), poly(propylene oxide) (PPO), and di‐epoxy and di‐amine monomer. The process of synthesis was very simple and green in ethanol as reactive media. These PEAs exhibit sharp response to temperature, pH, and ionic strength, with adjustable and sharp phase transitions in the range of 27–100 °C. The lower critical solution temperature (LCST) of PEA's aqueous solution presents a linear relationship to the PEO content (y = 35.7 + x), indicating well‐tunable LCST. The concentration of PEA has no obvious effect on LCST. Therefore, PEA will be potential in applications of drug delivery, separation, and biotechnology. © 2009 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 47: 1292–1297, 2009     

Characterization of chemical heterogeneity in polymer systems using hydrolysis and tapping‐mode atomic force microscopy

Characterization of polymer coatings microstructure is critical to the fundamental understanding of the corrosion of coated metals. An approach for mapping the chemical heterogeneity of a polymer system using chemical modification and tapping‐mode atomic force microscopy (TMAFM) is demonstrated. This approach is based on the selective degradation of one of the phases in a multiphase polymer blend system and the ability of TMAFM to provide nanoscale lateral information about the different phases in the polymer system. Films made of a 70:30 polyethyl acrylate/polystyrene (PEA/PS) blend were exposed to a hydrolytic acidic environment and analyzed using TMAFM. Pits were observed to form in the PEA/PS blend films, and this degradation behavior was similar to that of the PEA material. Using these results, the domains in the 70:30 blend were identified as the PS‐rich regions and the matrix as the PEA‐rich region. This conclusion was confirmed by Fourier transform infrared‐attenuated total reflection analyses that revealed the hydrolysis of the PEA material. TMAFM phase imaging was also used to follow pit growth of the blend as a function of exposure time. The usefulness of the chemical modification/AFM imaging approach in understanding the degradation process of a coating film is discussed. © 2001 John Wiley & Sons, Inc. J Polym Sci B Part B: Polym Phys 39: 1460–1470, 2001