Solid-phase synthesis of 6-hydroxy-2,4-diaminoquinazolines

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 X 22 compounds demonstrates the general utility of this approach. (c) 2005 Elsevier Ltd. All rights reserved.