The solid-phase synthesis of small organic molecules has received renewed a
ttention since the first reports of the polymer-supported synthesis of comp
ounds 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 original
ly for peptide synthesis, and the design and synthesis of new supports to p
ermit the anchoring and releasing of other functional groups. In this artic
le, resins and linkers are subdivided according to the functional group on
the solid support to which the first building block is anchored. The chemis
try of these supports is illustrated by a relatively small but representati
ve selection from the many recent examples of potential therapeutic agents
synthesized on solid supports. (C) 1999 John Wiley & Sons, Inc.