Polymer supports for solid-phase organic synthesis

Abstract

The solid-phase synthesis of small organic molecules has received renewed attention since the first reports of the polymer-supported synthesis of compounds of therapeutic interest. Solid-phase synthesis is now a key component of the high-throughput synthesis and screening approach to drug discovery. The recent rapid growth in the number of organic transformations that have been successfully demonstrated on solid supports has involved both the use of the established amine, halide, and hydroxyl supports developed originally for peptide synthesis, and the design and synthesis of new supports to permit the anchoring and releasing of other functional groups. In this article, resins and linkers are subdivided according to the functional group on the solid support to which the first building block is anchored. The chemistry of these supports is illustrated by a relatively small but representative selection from the many recent examples of potential therapeutic agents synthesized on solid supports. © 1999 John Wiley & Sons, Inc. Biopoly 47: 311–351, 1998