Development of New Supported Reagents for the Synthesis of Biologically Active Molecules
2008
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 solu- tion-phase chemistry, such as the ease of separation of the supported spe- cies 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 devel- oped 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.
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