Enriching chemical space with diversity-oriented synthesis: parallel synthesis of low molecular weight acyclic and heterocyclic compounds from resin-bound polyamides

Diversity-Oriented Synthesis (DOS), also known as combinatorial synthesis, is a process, by which multiple compounds are generated simultaneously, in a predictable fashion using techniques that involve parallel chemical transformations. Through diversity-oriented synthesis organic chemists are now able to achieve more structural complexity than in the early days of combinatorial chemistry. Combinatorial chemistry techniques offer unique enhancement in the potential identification of new and/or therapeutic candidates. Over the past fifteen years in the design and diversity oriented synthesis of low molecular weight acyclic and heterocyclic combinatorial libraries derived from amino acids, peptides and/or peptidomimetics are described. Employing a “toolbox” of various chemical transformations, the “libraries from libraries” concept has enabled the continued development of an ever-expanding, structurally varied, series of organic chemical libraries.