The invention provides an ultrasonic activated azido precursor, a
prodrug and application. The precursor and an active
drug react and are bonded to obtain the azido
prodrug; the bonding group of the active
medicine is amino, hydroxyl or sulfydryl; a bonding group of the ultrasonic activated azido precursor is an ester group. Novel ultrasonic activatable groups, namely p-azidobenzyloxycarbonyl and derivatives thereof, are adopted,
hydrogen atoms on a
benzene ring are substituted to different degrees, the
reducing capacity of a precursor can be remarkably improved,
azide is effectively reduced into amino through
ultrasonic stimulation under the action of TBR and NADH, and then a self-
elimination reaction is induced to release active drugs. The structure has the advantages that different types of active drugs (active pharmacodynamic groups can be amino, hydroxyl and sulfydryl) can be bonded through 4-nitrophenyl
carbonate, high-selectivity reduction is performed under the triple action of
ultrasound, TBR and NADH, active raw drugs are released according to needs, and
toxicity reduction and synergism are achieved.