Solid phase synthesis of mixture-based acyclic and heterocyclic small molecule combinatorial libraries from resin-bound polyamides

The development of soluble mixture‐based heterocyclic combinatorial libraries derived from amino acids and peptides is described. Starting with a “toolbox” of various chemical transformations, including alkylations, reductions, acylations, and the use of a variety of bifunctional reagents, the “libraries from libraries” concept has been expanded to encompass the development of more than fifty positional scanning combinatorial libraries each composed of tens of thousands of low molecular weight acyclic and heterocyclic compounds. © 2001 John Wiley & Sons, Inc. Biopolymers (Pept Sci) 60: 212–219, 2001