Efficient Multicomponent Synthesis of Biginelli-Dihydro-Pyrimidines and Evaluation of Anti-Cancer Activity

In the presence of imidazole hydrochloride, an efficient one-pot three-component synthesis of Biginelli reaction of aromatic aldehydes and aliphatic aldehydes, ethyl acetoacetate, and thiourea/urea was developed with good yields of dihydropyrimidines. High yields (80-95 %), mild reaction conditions, an easy work-up process, a fast reaction time and simple operations are all significant features of the reaction. A total of 15 dihydropyrimidines were synthesized and out of which 12 compounds were evaluated for their anti-cancer activity against cancer cell lines viz.A549, HT29, HepG2. Most of the synthesized compounds showed moderate to good anti-cancer activity (IC50=150>200 mu M).

Automated summary

In the presence of imidazole hydrochloride, an efficient one-pot three-component synthesis of dihydropyrimidines was developed with good yields. Most of the synthesized compounds showed moderate to good anti-cancer activity.