PROCESS FOR THE PREPARATION OF ETOPOSIDE PHOSPHATE AND INTERMEDIATES THEREOF

摘要

An etoposide phosphate represented by the formula (1): is prepared by blocking -the hydroxyl groups of the saccharide moiety of etoposide with halogenoacetyl groups, thereafter phosphorylating -the 4'-position, and removing the halogenoacetyl groups from the obtained phosphate in the presence of an amine. This precess can give the objective etoposide phosphate in a higher yield than that of the prior art to enable the industrial mass-production thereof.