固相有机合成:固相钯化学

P. Scott, D. Knight
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摘要

卡迪夫催化研究所,化学学院,卡迪夫大学,主要学院,公园广场,卡迪夫CF10 3AT,英国电子邮件:knightdw@cardiff.ac.uk这个相对较小的体积的目的是提供在固体支撑上进行钯催化偶联的代表性例子的方法,基本上是有机合成的风格(1)。学术和工业团体都有贡献。这是一个有点专业化的合成领域,需要在“正常”有机合成中使用的技术之外的技术。固相合成有许多优点和缺点。将候选药物的一部分固定在相当大的范围内的固体载体上,然后将药物靶标的一系列“第二”部分耦合到初始物种的样品上,这是一种非常方便和有吸引力的文库合成方法,而且可能非常有效和快速。或者,可以在固体载体上建立一系列不同的前体,然后使用钯催化进行循环。不利的一面是,跟踪这种合成的进展,并管理不同范围的反应物之间不可避免的反应速率差异,往往相当耗时。因此,本书的目的是提供一系列钯催化偶联反应的实验指导,这些反应对有机合成产生了重要影响。这些反应代表了当前对有机合成的看法和执行方式的真正范式转变。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
"Solid-Phase Organic Syntheses: Solid-Phase Palladium Chemistry"
Cardiff Catalysis Institute, School of Chemistry, Cardiff University, Main College, Park Place, Cardiff CF10 3AT, UK Email: knightdw@cardiff.ac.uk The purpose of this relatively small volume is to provide methods for carrying out representative examples of palladium-catalysed couplings on a solid support, essentially in the style of Organic Syntheses (1). There are contributions from both academic and industrial groups. This is a somewhat specialised area of synthesis, requiring techniques additional to those employed in ‘normal’ organic synthesis. Solid-phase synthesis has a number of pros and cons. The idea of immobilising part of, say, a drug candidate to a solid support on quite a large scale and then coupling a series of ‘second’ parts of the drug target to samples of the initial species can be a very convenient and attractive approach to library synthesis and one which is potentially very effi cient and rapid. Alternatively, a diverse series of precursors can be built up on a solid support then cyclised using palladium catalysis. On the downside, it is often rather time-consuming to follow the progress of such syntheses and to manage the inevitable differences in reaction rates between a diverse range of reactants. Hence, the purpose of this book is to provide experimental guidance across a range of palladiumcatalysed coupling reactions of the types which have made such an important impact on organic synthesis in general. These reactions represent a true paradigm shift in the way that organic synthesis is currently viewed and executed.
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来源期刊
Platinum Metals Review
Platinum Metals Review CHEMISTRY, PHYSICAL-
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