硝基取代肉桂酸合成方法的改进

对硝基取代肉桂酸的经典合成方法进行了改进，其反应条件温和、收率高、产品易于纯化精制和大规模生产。应用改进后的反应条件，合成了一系列硝基取代肉桂酸。     

氟合成技术在有机合成中的研究进展

１前言 根据反应介质的不同，有机反应可分为液相反应和固相反应，两者各有利弊。固相反应的分离纯化非常方便，简单的物理或化学方法就可达到目的。但是由于是在固相上反应，故反应类型的选择受到限制，并且对反应的跟踪也有一定困难。液相反应应用广泛，但是反应产物的分离难度较大，特别是在制备数目巨大的化合物库时更加困难。 近年来，人们一直在寻找一种有效的合成、分离方式，能将固相反应和液相反应的优点结合起来合成化合物。随着氟合成技术的出现和发展，它提供了一条有效可行的途径。２氟合成的基本原理 氟很强的电负性使得氟原…     

端基保护聚乙二醇ω-氨基酸的合成及表征

以聚乙二醇为原料,结合液相合成和固相合成方法合成了一种国内外尚未报道的端基保护聚乙二醇ω-氨基酸。目标化合物经红外光谱、核磁共振氢谱,质谱确证了其结构。本方法具有原料易得,反应条件温和,合成路线简短,分离纯化简单,产率高等优点。这种聚乙二醇ω-氨基酸可广泛应用于靶向药物合成,生物传感,免疫分析以及多肽合成等领域。     

纳米二硫化钼的合成与应用现状

纳米二硫化钼性能优越,用途广泛.介绍了纳米二硫化钼的3种合成方法:固相法、液相法、气相法.液相法中详细介绍了液相沉淀法、水热法和热溶剂法.另外介绍了纳米二硫化钼的应用研究现状,主要包括在润滑剂中和在复合材料中的应用研究.最后对纳米二硫化钼的合成及应用研究存在的问题及发展前景提出了看法.     

艾塞那肽的合成研究

艾塞那肽是胰高血糖素样肽-1（GLP-1）的类似物,由39个氨基酸组成,具有双激素靶向调控血糖的作用。本文对艾塞那肽的合成新方法进行了研究,将原肽拆分成六个全保护片段,分别经过独立的固相或液相方法合成,然后对片段进行组装,经切割、纯化,得到艾塞那肽产品0.98g,纯度﹥98%,总收率33.8%。切割时保留Fmoc-保护基可以使目标峰与杂峰有效分离。该方法结合了固相和液相合成的特点,与传统方法相比,是一种周期较短、纯化方便和收率较高的合成艾赛那肽的方法。     

纳米碳管

从纳米碳管的种类，合成，纯化，修饰以及应用方面对这种新型的纳米材料作了扼要的论述。     

月桂氮Zhuo酮的合成与应用

介绍了高效皮肤渗透促进剂月桂氮Ｚｈｕｏ酮的性能、合成工艺及应用，指出固－液相转移催化法是较好的生产方法。     

天冬氨酸寡肽的合成及表征

采用三氯氧磷辅助下,氨基酸自组装成肽的方法合成了天冬氨酸寡肽,并利用反相高效液相色谱法,采用优化了的色谱条件对产物进行了分离纯化,得到了纯度较高的寡肽产品天冬氨酸二肽和天冬氨酸三肽。天冬氨酸二肽和天冬氨酸三肽分别用质谱、红外和氢谱进行了结构表征。     

目标导向合成及差异导向合成在药物合成中的应用

介绍了目标导向合成和差异导向合成的基本概念,扼要阐述了目标导向合成在药物合成上的应用,着重综述了差异导向合成的固相有机合成法和液相有机合成法在合成有机小分子库以备药物筛选中的应用。认为差异导向合成在药物研究领域的作用必将变得更加重要。     

氰尿酸及三氯异氰尿酸的研究进展及现状

介绍了氰尿酸的两种合成路径 (固相法和液相法 ) ,三氯异氰尿酸的三种合成方法以及它们的应用 ;总结了这些合成方法的特点 ,并对它们的应用价值及国内外市场作了简要的说明     

组合化学及其在新农药开发中的应用

结合医药领域的成功经验概述了组合化学的基本概念、化合物库的合成技术与分析、筛选方法，综述了组合化学方法在发现与优化新农药先导化合物中的研究进展，介绍了作者利用互补分子反应活性与分子识别技术优化除草活性原卟啉原氧化酶抑制剂的研究工作，展望了组合化学在新农药创制中的应用前景。     

β-(对硝基苯基)-β-氨基丙酸合成方法的改进

在组合化学中 ,β (对硝基苯基 ) β 氨基丙酸是用于构建多肽化合物库的一种基本结构单元。通过对其合成方法中反应条件的改进即 :以乙酸代替乙醇做溶剂 ,反应温度为 95℃ ,预热溶剂并快速升温 ,使 β (对硝基苯基 ) β 氨基丙酸的产率从传统方法的 30 %左右提高到 60 %以上 ,且无需额外的纯化步骤即可得到质量分数大于 90 %的目标产品。     

合成化学新概念——组合化学

简明地介绍 2 0世纪 90年代刚刚问世的组合化学新概念以及组合合成基本方法 ,着重叙述了“一珠一肽”混合均分合成法的基本原理及其在新药合成及筛选研究中的应用 ,并对组合合成中编码技术作了初步介绍     

Solid phase synthesis – designer linkers for combinatorial chemistry: a review

Solid phase organic synthesis is a rapidly expanding area of synthetic chemistry which is being widely exploited in the search for new biologically active compounds by combinatorial techniques. This review introduces the key concepts of solid phase methodology and combinatorial synthesis with particular focus on the issues that concern the development of linkers which are used to attach the substrate to the solid support. © 1999 Society of Chemical Industry     

组合化学及其应用

组合化学是一种快速大量的合成技术。简明地介绍了组合化学的基本原理、化合物库的设计与制备方法、活性分子结构的表征以及组合化学在许多领域里的应用。     

Virtual Combinatorial Chemistry and Pharmacological Screening: A Short Guide to Drug Design

Traditionally, drug development involved the individual synthesis and biological evaluation of hundreds to thousands of compounds with the intention of highlighting their biological activity, selectivity, and bioavailability, as well as their low toxicity. On average, this process of new drug development involved, in addition to high economic costs, a period of several years before hopefully finding a drug with suitable characteristics to drive its commercialization. Therefore, the chemical synthesis of new compounds became the limiting step in the process of searching for or optimizing leads for new drug development. This need for large chemical libraries led to the birth of high-throughput synthesis methods and combinatorial chemistry. Virtual combinatorial chemistry is based on the same principle as real chemistry—many different compounds can be generated from a few building blocks at once. The difference lies in its speed, as millions of compounds can be produced in a few seconds. On the other hand, many virtual screening methods, such as QSAR (Quantitative Sturcture-Activity Relationship), pharmacophore models, and molecular docking, have been developed to study these libraries. These models allow for the selection of molecules to be synthesized and tested with a high probability of success. The virtual combinatorial chemistry–virtual screening tandem has become a fundamental tool in the process of searching for and developing a drug, as it allows the process to be accelerated with extraordinary economic savings.     

Simultaneous Disulfide and Boronic Acid Ester Exchange in Dynamic Combinatorial Libraries

Dynamic combinatorial chemistry has emerged as a promising tool for the discovery of complex receptors in supramolecular chemistry. At the heart of dynamic combinatorial chemistry are the reversible reactions that enable the exchange of building blocks between library members in dynamic combinatorial libraries (DCLs) ensuring thermodynamic control over the system. If more than one reversible reaction operates in a single dynamic combinatorial library, the complexity of the system increases dramatically, and so does its possible applications. One can imagine two reversible reactions that operate simultaneously or two reversible reactions that operate independently. Both these scenarios have advantages and disadvantages. In this contribution, we show how disulfide exchange and boronic ester transesterification can function simultaneous in dynamic combinatorial libraries under appropriate conditions. We describe the detailed studies necessary to establish suitable reaction conditions and highlight the analytical techniques appropriate to study this type of system.     

Generation of a Multicomponent Library of Disulfide Donor-Acceptor Architectures Using Dynamic Combinatorial Chemistry

We describe here the generation of new donor-acceptor disulfide architectures obtained in aqueous solution at physiological pH. The application of a dynamic combinatorial chemistry approach allowed us to generate a large number of new disulfide macrocyclic architectures together with a new type of [2]catenanes consisting of four distinct components. Up to fifteen types of structurally-distinct dynamic architectures have been generated through one-pot disulfide exchange reactions between four thiol-functionalized aqueous components. The distribution of disulfide products formed was found to be strongly dependent on the structural features of the thiol components employed. This work not only constitutes a success in the synthesis of topologically- and morphologically-complex targets, but it may also open new horizons for the use of this methodology in the construction of molecular machines.     

组合化学在农药合成中的应用进展

本文综述了组合化学的发展历史、原理、在农药合成中的应用情况及前景。     

Dynamic Combinatorial Chemistry in Chemical Catalysis

Despite the progress in the field of dynamic combinatorial chemistry (DCC), dynamic combinatorial catalysis has received considerably less attention. Some first studies, however, have provided proof of principle and demonstrated that DCC-based approaches are also applicable in catalyst development. This provides interesting new tools that are complementary to rational catalyst design and traditional combinatorial strategies. As such, DCC may become highly valuable in the field of dynamic combinatorial catalysis, due also to the practical importance of catalysis. In this review we focus on the principles of dynamic combinatorial catalysis and provide an overview by the introduction of different concepts related to the development of libraries and selection procedures in catalysis.