Highly convergent Synthesis of-aminophosphonates were most conveniently achieved using organophosphorus chemistry. Synthesis of-aminophosphonates were accomplished by three-component coupling of carbonyl, amine and hydrophosphoryl compounds. These aminophosphonates exhibited promising antimicrobial, antioxidant and anticancer activity. Some recent developments and applications to the synthesis of biologically activeaminophosphonates are also included.