CYTOSTATIC VINBLASTINE COMPOUNDS AND PROCESSES FOR THEIR PREPARATION

摘要

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 /I/ in which R4 is .beta.-hydroxyl and R3 is ?-ethyl; or R4 is hydrogen and 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 group haa 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 thai if R3 is .alpha.-ethyl and R4 .beta.-hydroxyl, R4 is other than ethyl. These compounds and N-desmethyl-N-ethoxymethyl-vinblastine can be prepared according to the invention by transetherification of compounds of the compounds of the general formula (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.