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Chemistry of biologically active dihydropyrimidones of Biginelli type compounds

Bahar Ahmed, Manoj Keshari, Habibullah

One pot cyclocondensation of â-keto ester, urea and aromatic or aliphatic aldehyde in ethanolic solution in presence of acid catalyst leads to the synthesis of 4-aryl-3, 4- dihydropyrimidines- 2(H)-ones. The reaction is called as Biginelli reaction. The classical reaction was modified by several researchers by using different catalysts and several structural variants to synthesize large number of Biginelli type compounds possessing a wide range of pharmacological activity namely anti-inflammatory, antimicrobial, anticancer,  adrenergic antagonistic, anti HIVCD 4 cell inhibitor, and cardiovascular etc. The present reviewis a complete compilation of literature available related to large number of Biginelli type compounds possessing different biological activities, with a focus on various advance synthetic methods, mechanistic approach, stereochemical aspects, and conformational studies.