An efficient green multi-component reaction strategy for the synthesis of highly functionalised pyridines and evaluation of their antibacterial activities

Abstract

An efficient green multi-component reaction (MCR) method has been developed for the synthesis of 2-amino-4-aryl/heteroaryl-6-(pyridin-2-ylthio)pyridine-3, 5-dicarbonitrile(s) via a 3-component reaction of aryl aldehyde(s), malononitrile and 2-mercaptopyridine in the presence of K2CO 3 under solvent free reaction conditions (SFRC) using grinding technique at room temperature in a single step. The advantages of the present protocol is operationally simple, environmentally benign, solvent-free reaction conditions (SFRC), simple work up, excellent isolated yields of desired products and viable method for large scale applications in pharmaceutical industry. Interestingly, the synthesized compounds showed moderate to excellent antibacterial activities against Gram-positive and Gram-negative bacterial strains. © 2013 The Pharmaceutical Society of Japan.