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Pure Appl. Chem. 76(5), 1017-1024, 2004

Pure and Applied Chemistry

Vol. 76, Issue 5

Solid- and solution-phase synthesis of bioactive dihydropyrimidines

D. Dallinger, A. Stadler, and C. O. Kappe

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

Abstract: With the emergence of high-throughput screening in the pharmaceutical industry over a decade ago, synthetic chemists were faced with the challenge of preparing large collections of molecules to satisfy the demand for new screening compounds. The unique ex-
ploratory power of multicomponent reactions such as the Biginelli three-component reaction was soon recognized to be extremely valuable to produce compound libraries in a time- and
cost-effective manner. The present review summarizes synthetic advances from our laboratories for the construction of Biginelli libraries via solution-and solid-phase strategies that
are amenable to a high-throughput or combinatorial format.

*Lecture presented at the Polish-Austrian-German-Hungarian-Italian Joint Meeting on Medicinal Chemistry, Kraków, Poland, 15-18 October 2003. Other presentations are published in this issue, pp. 907 -1032.

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