A method for the aralkylation of anthracyclins by utilizing an
aralkylating agent R.sub.3-CH.sub.2X (for example, BnBr) in accordance
with the reaction pathway describe by the scheme shown in FIG. 1. The
present invention recognizes that 4-R.sub.1, 3'-N.sub.3-Daunomycines are
suitable substrates for selective 4'-O-benzylation, yielding 4-R.sub.1,
3'-N.sub.3-4'-O-Aralkyl-Daunorubicines (in particular,
4'-O-Bn-Daunomycines). Thus, the present invention provides a pathway for
a simple production of 4'-O-aralkylated derivatives of anthracyclines
which can be effectively used to produce anthracyclines.