One-pot and catalyst-free synthesis of novel α - aminophosphonates under microwave irradiation and their Bioactivity

A simple and an efficient synthetic protocol were adopted for the synthesis of novel αaminophosphonates derivatives containing pyrazine moiety such as diethyl phenyl (pyrazin-2-yl-amino) methylphosphonates (4a-l) through one-pot three component Kabachnik-Fields reaction. Pyrazino-2-amine (1), different substituted aldehydes and triethyl phosphite (3) were reacted in toluene under microwave irradiation without catalyst to obtain title compounds. The newly synthesized compounds were screened for their in vitro antibacterial activity (Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, and Salmonella typhimurium) and antifungal activity (Candida albicans, Aspergillus niger).