Eco-friendly synthesis of 2-azetidinone analogs of isonicotinic acid hydrazide

摘要

2-Azetidinones possess broad and potent activity due to presence of β-lactam ring and has been established as one of the biologically important scaffolds. The synthesis of N-(4-aryl-2-oxoazetidinone)-isonicotinamide by novel methods of stirring and sonication are described. The conventionalmethod for synthesis of 2-azetidinones involves use of Dean Stark water separator for the removalof water from the reaction with long reaction time (12-16 h reflux) at a very low temperature (-70 to -90°C). The microwave method reported requires inert atmosphere of nitrogen gas for the synthesis of 2-azetidinones. We report herein the synthesis of 2-azetidinone analogs of isonicotinic acid hydrazide by novel green route methods of sonication and stirring using molecular sieves. Results indicate that higher yields and shorter reaction times can be achieved by employing novel green route methods of synthesis.