Process for preparing 4'-haloanthracycline glycosides

C - Chemistry – Metallurgy – 07 – H

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260/208.2

C07H 15/252 (2006.01)

Patent

CA 1250833

\ ABSTRACT OF THE DISCLOSURE A process for preparing 4'-halo-anthracycline glycosides having general formula A : Image A in which X=H or OH, R1=H, OH or OCH3, R2=Br, Cl or F 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 C5F. Those in which X=OH are prepared from those in which X=H by bromination and reaction with aqueous sodium formate.

460796

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