"Solid-Phase Organic Syntheses: Solid-Phase Palladium Chemistry"

Abstract

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.