abstract |
The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula <IMAGE> (I) in which R4 is beta -hydroxyl and R3 is alpha -ethyl; or R4 is hydrogen and R3 is beta -ethyl; R'' is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >Na-CH2-O- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety; R1 is methoxy and R2 is acetyl, provided that if R3 is alpha -ethyl and R4 beta -hydroxyl, R4 is other than ethyl. These compounds and N-desmethyl-N- ethoxy- methyl -vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula <IMAGE> (II) with a large excess of alcohols of the general formula R''-OH (III) Pharmaceutical compositions containing compounds of the general formula /I/ as active ingredients are also within the scope of invention. |