A microwave assisted green synthetic methodoloy was developed for the
synthesis various substituted pyrrolidinones derivatives by the one-pot three component
reaction of aromatic aldehydes, aniline with dialkylbut-2-ynedioate in the presence of p-TsOH
in water medium. The compounds were screened for their in vitro antimicrobial activity
against four bacterial organism and two fungal organisms, resulted moderate to good activity
with compared to their standard drug.
A series of novel carbohydrazide and carboxamide derivatives of hetero-fused pyridine derivatives
were synthesized starting from bis-trifluoromethyl containing pyridine 1. Compound 1 on Smiles
rearrangement obtained compound 2, then compound 2 on coupling with diethyl
ethoxymethylenemalonate (EMME), further reaction with POCl3 and hydrazine hydrate to obtain
pyridopyrimidine hydrazide derivatives. This hydrazide derivative reacts with different substituted
aromatic aldehydes to produce title carbohydrazide derivatives 6a-h. Pyridopyrimidine carboxylate
compound on reaction with aliphatic amine to obtain carboxamide derivatives 7a-e. All the final products
evaluated for their anticancer activity, against four human cancer cell lines and promising compounds
have been identified. Compounds 7a and 7b exhibits remarkable activity.
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