Patented Catalysts for the Synthesis and Biological Applications of Dihydropyrimidinones: Recent Advances of the Biginelli Reaction
Ricardo A. W. Neves Filho, Martin C. N. Brauer, Mieder A. T. Palm-Forster, Ronaldo N. de Oliveirac and Ludger A. Wessjohann
Affiliation: Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, 06120 Halle (Saale), Germany.
Keywords: Biginelli reaction, biological activity, cancer, catalyst, dihydropyrimidine, dihydropyrimidinones, HIV, Lewis acid, monastrol, thermal condensation.
The acid-catalyzed and thermal multicomponent cyclocondensation between an aldehyde, a beta-keto ester and
urea to generate dihydropyrimidinones (DHPMs) is one of the best studied multicomponent reactions in organic synthesis.
It is frequently employed in the synthesis of natural products and biologically active compounds. After several years under
academic development, this reaction drew the attention of researchers in the chemical and pharmaceutical industry.
This critical review is focused on the development and applications of the Biginelli three component reaction (B-3CR)
patented in the last three decades.
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