Pd‐mediated construction of pyridine scaffold and subsequent Suzuki‐based C—C coupling reaction in one pot has been accomplished for the synthesis of 4‐biaryl substituted 2‐amino‐3‐cyanopyridines via multicomponent reaction. The present multicomponent reaction is useful in structural elaboration of pyridine framework and also helpful in design and synthesis of novel and diverse analogs of complex heterocyclic compounds other than present reported molecules. Antibacterial activities of the synthesized compounds were systematically evaluated. The correlation between functional group variation and biological activities of the compounds has been evaluated against human pathogenic gram‐positive and gram‐negative bacterial strains.
Bromination of aralkyl ketones using N-bromosuccinimide in presence of active Al2O3 provided either α-monobrominated products in methanol at reflux or mononuclear brominated products in acetonitrile at reflux temperature with excellent isolated yields depending on the nature of substrate employed. The α-bromination was an exclusive process when aralkyl ketones containing moderate activating/deactivating groups were subjected to bromination under acidic Al2O3 conditions in methanol at reflux while nuclear functionalization was predominant when aralkyl ketones containing high activating groups were utilized for bromination in presence of neutral Al2O3 conditions in acetonitrile at reflux temperature. In addition, easy isolation of products, use of inexpensive catalyst, short reaction time (10–20 min), and safe operational practice are the major benefits in the present protocol.
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