abstract |
Process for preparing hydroxy-9-ellipticin and derivatives with the following general formula (FORMULA) in which R1 represents hydrogen or an alkyl group and R2 represents hydrogen or an alkyl, aryl, benzyl or benzoyl group, as well as quaternary salts, by the condensation of methoxy-5-indole with hexane-dione 2,5 in order to obtain methoxy-6-dimethyl-1,4-carbazole, followed by demethylation, the protection of the hydroxy group and, eventually, the alkylation of the nitrogen atom and then formylation, condensation of the aminoacetaldehyde with dimethylacetal, cyclisation and removal of the protective group. The ellipticin derivatives thus obtained are extremely pure and can be utilised in the treatment of cancers. |