A new method for the solid-phase synthesis of 6-hydroxy-2, 4-diaminoquinazolines has been developed. The synthesis utilizes solid-phase bound 6-hydroxy-2, 4- dichloroquinazoline as a key intermediate. Sequential substitution of the two chlorines furnishes the title compounds regioselectively with high purity. A library of 18× 22 compounds demonstrates the general utility of this approach.