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.

Biginelli reaction, biological activity, cancer, catalyst, dihydropyrimidine, dihydropyrimidinones, HIV, Lewis acid, monastrol, thermal condensation.

Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, 06120 Halle (Saale), Germany.