Abstract
13H-quinazolino[3,4-a]quinazolin-13-ones have been synthesized from 2-aminobenzamides in four steps. An acid-catalyzed or base-catalyzed isomerization of 13H-quinazolino[3,4-a]quinazolin-13-ones to 8H-quinazolino[4,3-b]quinazolin-8-ones in excellent yields (90–95%) has been reported. The differences in the infrared and nuclear magnetic resonance (1H & 13C) data of these isomeric fused quinazolinoquinazolinones afford a useful method for distinguishing between the two series. These analogs showed moderate anticancer activity (EGFR-TK inhibition).
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