The synthesis of some potentially active 2-(trifluoromethyl)pyrimido[1,2-a]benzimidazoles and pyrimido[1,2-a]benzimidazol-2(1H)-ones by the cyclization of 4-alkoxyvinyl trifluoro(chloro)methyl ketones with 2-aminobenzimidazole is described. The structure of the products was assigned based on 1H and 13C NMR as well as 2D-NMR experiments. Some of the obtained products exhibited significant DNA-topoisomerase I inhibitory activity.
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Zanatta et al. (2006) studied this question.
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