The Solid-Phase Part of Supported Small-Molecule Synthesis

Abstract

The synthesis of small molecules on solid phase must not only address the vagaries of C–C-bond formation and functional-group manipulation, but must also take into account solid-support issues such as 'point of attachment', 'resin compatibility', 'reagent accesibility', and 'product liberation'. Hence, the resin plays a vital role in the solid-phase venture and the polymer advantages can be summarized as reactions can be driven to completion by addition of excess solution-phase reagents, reaction products are 'isolated' by filtration and washing, and multiple-step synthesis terminating with a 'selective' liberation step can deliver essentially pure product. These issues, as well as a number of strategies for the preparation and functionalization of resin supports, are discussed.