A simple, efficient one-pot synthesis of 2-isoxazoline derivatives and their antimicrobial activity

Synthesis of substituted 2-isoxazolines derivatives with sulfone functional groups was accomplished by 1,3-dipolar cycloaddition reaction. The 1,3-dipolar nitrile oxides generated in situ by reacting α-formaldoximes with N-bromosuccinimide in the presence of triethylamine on reaction with activated alkenes in toluene at room temperature afford the corresponding 2-isoxazolines in high yields. All the 2-isoxazoline derivatives were assayed for their antibacterial activities against Staphylococcus aureus, Bacillus cereus, Escherichia coli, and Pseudomonas aeruginosa and antifungal activities against Aspergillus niger and Candida albicans. Most of the compounds showed good antibacterial and antifungal activities.