The Biginelli Reaction is a one-pot acid catalysed cyclocondensation of -keto ester, urea and aromatic aldehyde which leads to the synthesis of functionalised 3,4-dihydro-2(H)-pyrimidinones (DHPMs). This three-component reaction for the synthesis of dihydropyrimidinone and corresponding dihydropyrimidinethiones has now been known for more than a century since first reported in 1893. The classical reaction has been modified in the recent past by using various catalysts and several structural variants in different solvents to synthesize large number of Biginelli type compounds. Also, these DHPMs (synthetic and natural) possess a wide range of pharmacological activities. Manuscript profile