Combinatorial Chemistry: Concepts, Strategies and Applications

Evelyn B. Rodriguez
Institute of Chemistry
University of the Philippines Los Baños

http://doi.org/10.57043/transnastphl.2001.5139

Abstract

Combinatorial chemistry started with Merrifield’s Nobel Prize-winning invention: the solid-phase synthesis of peptides. By the mid-1980s, solid-phase techniques had been greatly refined, so that it was possible to make huge numbers of peptides simultaneously in the same reaction vessel, using a few steps. Later, strategies and techniques of solution-phase combinatorial synthesis were developed as well. While solid-phase synthesis makes it easier to conduct multi-step reactions and to drive reactions to completion, solution-phase synthesis allows a much wider range of organic reactions.

In its earliest form, the primary objective of combinatorial chemistry was to generate large “libraries” of molecules en masse—instead of synthesizing compounds one by one, as synthetic organic chemistry had been practiced for the last 100 years—and to find the most promising “lead” pharmaceutical compounds by high-throughput screening of the libraries. Although combinatorial chemistry and combinatorial technology have been mostly applied to drug and agrochemical discovery, they can be powerful tools in the diagnostic, downstream processing, catalysis, and new materials sectors.