Generation of 500-member library of 10-alkyl-2-R1,3-R 2-4,10-dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones

Abstract

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-a]pyriminin-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.