Combinatorial chemistry

Gordon Lowe
Chem. Soc. Rev., 1995, 24, 309-317
https://doi.org/10.1039/CS9952400309

Abstract

Combinatorial chemistry is a novel and innovative way of rapidly generating a large number of related compounds. The solid phase method of synthesis, first introduced by Merrifield for peptide synthesis some 30 years ago, is generally used for preparing combinatorial chemical libraries. The solid phase method has many advantages over solution phase chemistry, most notably that excess reagents may be used to drive reactions rapidly to completion and then by-products and excess reagents removed by a simple washing procedure. The whole process is capable of automation and instrumentation is commercially available for this purpose. Although the solid phase method of synthesis initially received much criticism, primarily because intermediates are not characterized, as reagents and protecting groups for peptide synthesis improved and the purification of peptides by HPLC became routine, the method was accepted as the preferred method of peptide synthesis. The solid phase method has also been successfully developed for the synthesis of oligonucleotides which are now routinely used in molecular biology.

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