The Biginelli reaction is a cyclo-condensation process that is one-pot acid-catalyzed and produces functionalized DHPMs by combining urea, [Formula: see text]-keto ester, and aromatic aldehyde. This three-component reaction was reported in 1893 and has been acknowledged for over a century as a means of synthesizing dihydropyrimidinone and related dihydropyrimidinethiones. The necessity for sustainable chemistry and the growing usage of green technology approaches have led to a renewed interest in this reaction to produce DHPMs with higher yields while also being environmentally conscious. Recently, many Biginelli-type compounds have been synthesized by modifying the classical reaction utilizing different catalysts and structural variants in different solvents. This paper briefly discussed the literature on preparing DHPMs using different methods and techniques along with their biological activities.