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首页> 外文会议>NATO Advanced Study Institute on New Methodologies and Techniques for a Sustainable Organic Chemistry: Sustainable Development in a Secure Environment Certosa di Pontignano; 20051014-23; Siena(IT) >DEVELOPMENT OF NEW SUPPORTED REAGENTS FOR THE SYNTHESIS OF BIOLOGICALLY ACTIVE MOLECULES
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DEVELOPMENT OF NEW SUPPORTED REAGENTS FOR THE SYNTHESIS OF BIOLOGICALLY ACTIVE MOLECULES

机译：用于合成生物活性分子的新型支持试剂的开发

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摘要

As a consequence of the changes associated with the need for preparing arrays of compound for hit discovery in pharmaceutical and fine chemical research laboratories, the research of new technologies that allow for the automation of synthetic processes has been developed. Since the pioneering work by Merrifield, polymeric supports have played a key role in this field. Polymer assisted solution-phase synthesis, which utilizes immobilized reagents and catalysts has more recently entered in the organic chemistry laboratories. It has various advantages over conventional solution-phase chemistry, such as the ease of separation of the supported species from a reaction mixture by filtration and washing and the opportunity to use an excess of the reagent to force the reaction to completion. On the other hand, as the reactions are performed in solution, the analytical techniques are the same of conventional synthesis. Various strategies for employing functionalized polymers stoichiometrically have been developed and this chapter reports some selected examples of use of reagents covalently attached to the polymeric backbone. This selection is intended to attract synthetic chemists to use this technique highlighting the use of the methodology to solve synthetic problems and pointing out which reagents and scavengers may have potential applications in sustainable and more secure chemical processes.
机译：由于与在制药和精细化学研究实验室中制备用于命中发现的化合物阵列有关的变化，已经开发了允许合成过程自动化的新技术的研究。自Merrifield的开创性工作以来，聚合物载体在该领域发挥了关键作用。利用固定化试剂和催化剂的聚合物辅助溶液相合成最近已进入有机化学实验室。与常规的溶液相化学方法相比，它具有多种优势，例如，易于通过过滤和洗涤从反应混合物中分离负载的物质，并有机会使用过量的试剂来迫使反应完成。另一方面，由于反应在溶液中进行，因此分析技术与常规合成相同。已经开发了各种化学计量地使用官能化聚合物的策略，并且本章报告了一些选择使用共价连接到聚合物骨架上的试剂的例子。该选择旨在吸引合成化学家使用该技术，强调使用该方法来解决合成问题，并指出哪些试剂和清除剂可能在可持续且更安全的化学过程中具有潜在的应用。

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