AN EFFICIENT SYNTHESIS AND ANTIBACTERIAL SCREENING OF NOVEL OXAZEPINE alpha-AMINOPHOSPHONATES BY ULTRASOUND APPROACH

An efficient synthesis of novel alpha-aminophosphonates by the reaction of quino[2,3-b][1,5]benzoxazepines with triethyl phosphite in the presence of the easily available, inexpensive, and nontoxic catalyst p-toluene sulphonic acid (p-TSA). This method affords the alpha-aminophosphonates under the influence of ultrasound irradiation in solvent-free conditions, in short reaction times (4-6 min), high yields (80-90%), with improved purity. The synthesized alpha-aminophosphonates show antibacterial activity against Gram-positive and Gram-negative bacteria.