PURPOSE: To provide a new 8-fluoroanthracyclin glycoside deriv. which is increased in the activity and selectivity of the known glycoside having an antitumor property and has the excellent antitumor property and also provide the pharmaceutically permissible salt thereof.
CONSTITUTION: This invention relates to the compd. of formula I (R is H, OH, OR"; R1 is H, OH, OCH3; R" is CHO-COCH3, acyl residue derived from ≤6C carboxylic acid; wave lines indicate that MH2 can be axial arrangement or equatorial arrangement) and the pharmaceutically permissible salt thereof; for example, 4-demthoxy-8-fluoro-3'-diamino-4'-deoxy-4'-4'-epi-amino daunorubicin hydrochloric salt. The compd. in which R is H is obtd. by bringing the compd. of formula II into condensation with the compds. of formulas III to IV (R2 is NHCOCF3, allyloxycarboxyamide), then removing an N-protective group.
LOMBARDI PAOLO (IT)
ARCAMONE FEDERICO (IT)
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