Combination with high throughput screening, combinatorial organic synthesis of diverse libraries of biologically active compounds has revolutionized the drug discovery process. Although combinatorial organic synthesis on solid supports is a useful approach, several groups are focusing their research efforts on liquid-phase combinatorial synthesis by using soluble polymer supports for generation of libraries. This macromolecular carrier (PEG), in contrast to an insoluble matrix, is soluble in different kinds of organic solvents and has a strong tendency to precipitate in some particular solvents. Liquid-phase combinatorial synthesis is a unique approach since homogeneous reaction conditions can be applied, while product purification similar to the solid-phase method can be carried out by simple filtration and washing. This strategy retains the advantages of classical solution-phase chemistry and solid-phase polymer-supported synthesis. Moreover, the smart designation of traceless linkers approach and the utilization of microwave technology on combinatorial chemistry improve the reaction's condition, time and results. This review, first, presents the history of soluble polymer supports in the synthesis of combinatorial libraries; and then, some selected examples from our laboratory are introduced.
|Number of pages||48|
|Journal||Chinese Pharmaceutical Journal|
|State||Published - 1 Dec 2003|
- Parallel synthesis
- Soluble polymer supports