PROCESS FOR PREPARING 4-HALO-ANTHRACYCLINE GLYCOSIDES

摘要

Compounds of the above formula (X=H or OH, R1=H, OH or OCH3, R2=Br, Cl or F) and their acid addition salts are useful as antitumour agents. Those in which X=H may be prepared by an exchange reaction between a 4'-epi-4'-O-trifluoromethanesulphonyl-N-protected-daunorubicin (or a corresponding 4-demethyl or 4-demethoxy derivative) and (C4H9)4NCl, (C4H9)4NBr or CsF. Those in which X=OH are prepared from those in which X=H by bromination and reaction with aqueous sodium formate.