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.