Generation of 500-member library of 10-alkyl-2-R(1),3-R(2)-4,10-dihydrobenzo[4,5]imidazo[1,2-alpha]pyrimidin-4-ones.

Representative benzimidazopyrimidinones were previously reported to be intercalating antitumor agents. In this work, we used 2-substituted 4,10-dihydrobenzo [4,5]imidazo[1,2-alpha]pyrimidin-4-ones for their diversification by regioselective alkylation. Under the conditions established, the alkylation gave 10-alkyl derivatives which permitted the parallel generation of a 500-member library of the title compounds.