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Pure Appl. Chem., 2005, Vol. 77, No. 1, pp. 155-161

Creating chemical diversity space by scaffold decoration of dihydropyrimidines

Doris Dallinger and C. Oliver Kappe*

Institute of Chemistry, Karl-Franzens-University Graz, Austria

Abstract: 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. The focus of this article will be on the scaffold decoration of biologically active dihydropyrimidines (DHPMs) of the Biginelli type, exploring the diversity on all six positions around the scaffold. This opens up the generation of a very large number of analogs given the commercial availability of the building blocks that are used in the functionalization process.