Microwave-assisted synthesis of -CF3 functionalized 3,4-dihydropyrimidinone/thione/imine derivatives by using potassium phthalimide (PPI) as a green and reusable organocatalyst and their anti-microbial evaluation

Abstract

One-pot synthesis of novel -CF₃ functional group containing 3,4-dihydropyrimidinone/thione/imine derivatives 8a-l, 9a-l and 10a-l has been successfully performed in high yields through the reaction of aromatic aldehydes, β-dicarbonyl compound, urea/thiourea/guanidine hydrochloride by using potassium phthalimide (PPI) as organocatalyst under solvent-free conditions under microwave irradiation at 300 W. PPI has been introduced as an efficient and biodegradable organocatalyst in Biginelli condensation with excellent reusability. The good yield of products, fast reaction time, simple work-up procedure, as well as usage of nontoxic, reusable, and easily recoverable catalyst under magnetic starring have been counted as advantages of the applied process. This organocatalyst can be removed after completion of reaction and reused several times under the same reaction conditions without significant loss of catalyst activity. The anti-microbial activity of all newly synthesised Biginelli products has been investigated against a variety of microorganisms such as E. coli, S. aureus, S. pyogenes, P. aeruginosa, C. albicans, A. niger and A. clavatus.