seen framstella cytostatic foreningar comprising derivatives of vinblastine and leurosidin jemte pharmaceutical preparations derav

摘要

A process for the preparation of new cytostatic compounds of general formula (I IMAGE in which either R4 represents a beta -hydroxyl group and R3 represents an alpha -ethyl group or R4 represents a hydrogen atom and R3 represents a beta -ethyl group; R'' represents a methyl group, a straight chain alkyl group having from 3 to 10 carbon atoms, a branched chain alkyl group having from 3 to 10 carbon atoms and in which the carbon atom attached to the IMAGE group has a primary or secondary configuration, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety; R1 represents a methoxy group; and R2 represents an acetyl group; which comprises reacting a compound of formula (II), IMAGE (in which R1, R2, R3 and R4 are as defined above), or an acid addition salt thereof with a large excess of an alcohol of formula R''-OH (III (wherein R'' is as defined above) in the presence of chromium trioxide at a temperature of from -60 DEG C to -30 DEG C.