High-Speed Organic and Medicinal Chemistry using Microwave Heating

Tuesday, May 30, 2006 Print

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The demand for diverse compound libraries for screening in drug discovery and materials science is the driving force behind the development of new technologies for rapid parallel and combinatorial synthesis. One of those high-speed techniques is microwave-assisted organic synthesis which has attracted a substantial amount of attention in the last few years [1].

The main benefits of performing reactions under microwave irradiation conditions are the significant rate-enhancements and the higher product yields that can frequently be observed. Not surprisingly, these features have recently also attracted interest from the drug discovery/medicinal chemistry communities where reaction speed is of great importance. The combination of microwave heating technology and combinatorial chemistry applications therefore seems a logical consequence of the increased speed and effectiveness offered by using microwave irradiation instead of conventional heating methods.

The focus of this lecture will be on microwave-assisted solid-phase synthesis, multicomponent reactions, and solution-phase library generation strategies using automated sequentialmicrowave irradiation techniques. Recent trends in reactor design suitable for scale-up and process research will also be highlighted.

[1] Kappe, C. O. "Controlled Microwave Heating in Modern Organic Synthesis”, Angew. Chem. Int. Ed. 2004, 43, 6250. Kappe, C. O.; Stadler, A. "Microwaves in Organic and Medicinal Chemistry", Wiley-VCH, 2005.