Efficient regioselective synthesis of 6-amino-5-benzoyl-1-substituted 2(1H)-pyridinones

A regioselective and efficient approach towards 6-amino-5-benzoyl-1-substituted 2(1H)-pyridinones by reaction of acyclic ketene aminals with propiolic acid ester is developed. The effect of the solvent and temperature on the radioactivity of the reaction and the compatibility of the target compounds to functional group manipulations is examined.