The Biginelli reaction is considered one of the well-known examples of a
multicomponent reaction that is useful in the synthesis of dihydropyrimidinones
(DHPMs) using aryl aldehydes, urea, and esters and these are significant compounds in
medicinal chemistry and chemical synthesis. DHPMs are considered vital compounds
due to their diverse biological functions. Because of their remarkable and concentrated
target-oriented biological activity, DHPMs have been the subject of large-scale and
extensive research in the past few decades to determine how to synthesize them by
using various catalysts and structural variations in a variety of solvents. Ionic liquids,
Lewis acids, and organocatalysts are some of the chiral catalysts used in the
enantioselective Biginelli reaction. This book chapter summarizes chiral reagents for
asymmetric synthesis with particular absolute configuration.
Keywords: Asymmetric synthesis, Biologically activities, Chirality, Dihydropyrimidinones, Enantioselectivity, Medicinal chemistry.
