8-FLUOROANTHRACYCLINE GLYCOSIDES OR PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, METHOD OF PREPARATION THEREOF, PHARMACEUTICAL COMPOSITION, INTERMEDIATE COMPOUNDS, AND METHOD OF PREPARATION THEREOF Russian patent published in 1997 - IPC

FIELD: pharmaceutical industry. SUBSTANCE: present invention describes novel anthracycline glycoside 8-fluoroderivatives of general formula: wherein R is H or OH; R₁- is H, OH or MeO; and wherein X is chlorine or p-nitrobenzoyloxy group; R₂ is trifluorocarbomamide or allyloxycarboxyamide group followed by removal of protecting groups, and optionally transformation of R hydrogen to R hydroxy through corresponding 14-bromoderivative. Present invention describes intermediate compounds IIIa and IIIe and method of preparation of said compounds. The claimed method comprises reacting methyl -2,3,6-trideoxy-α-L- glycerohexoxy pyranoside-4-ylose with hydroxyamine, followed by reducing the resulting mixture of syn-and antioximes, protecting the resulting amino group and separating corresponding epimers and subsequently transforming the latter into corresponding 1- hydroxyderivatives and the desired product. Present invention also describes intermediate compounds of formula II and VII: wherein R is H, OCH₃ or OH, and pharmaceutical composition. Compounds have antitumor properties. EFFECT: improved properties of the pharmaceutical composition. 17, 4 tbl