Synthesis of N-(4-bromo-2-trifluoromethylphenyl)-1-(2-fluorophenyl)-O,O-dialkyl-α-aminophosphonates under ultrasonic irradiation

Boron trifluoride diethyl etherate catalyzes the Mannich-type reaction of 2-trifluoromethyl-4-bromoaniline and O,O-dialkylphosphite with 2-fluorobenzoaldehyde under ultrasonic irradiation to synthesize the corresponding product α-aminophosphonate. The advantages of the procedure include short reaction period, high yield and simple working up. Their structures were clearly established by IR, 1H NMR, 13C NMR and elemental analysis. The bioassay tests showed that the title compounds exhibit moderate antitumor activity in vitro by MTT method.