SEMISYNTHETIC DIASTEREOMERICALLY PURE N-GLYCIDYL- ANTHRACYCLIN, METHOD OF STEREOSELECTIVELY MANUFACTURING SAME AND USE THEREOF AS CELL PROLIFERATION INHIBITOR

The invention relates to anthracyclines with cytostatic activity and the formula I, which are optionally in the form of a salt of an inorganic or organic acid, in which R is hydrogen or a hydroxyl group, R is hydrogen, a hydroxyl group or an alkyloxy group (C1-C4), R is hydrogen, a hydroxyl group or...

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Hauptverfasser: MANFUREETO GERUKEN, ERUNSUTO RAAPU, RAINAA SHIYUTORAUPU, DEIITAA HOFUMAN, MONIKA GURIMU
Format: Patent
Sprache:eng
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Zusammenfassung:The invention relates to anthracyclines with cytostatic activity and the formula I, which are optionally in the form of a salt of an inorganic or organic acid, in which R is hydrogen or a hydroxyl group, R is hydrogen, a hydroxyl group or an alkyloxy group (C1-C4), R is hydrogen, a hydroxyl group or a structure of the formula II, R is CH2CH3, COCH3, COCH2OH, CHOHCH3 or CHOHCH2OH, R is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II, R is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or dimethyloxy-substituted benzyl group, a tetrahydropyranyl group, R is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or dimethyloxy-substituted benzyl group, and R is a structure of the formula III or IV, and to a process for the preparation of these compounds, characterised in that an anthracycline derivative of the structure I in which R , R and R are as defined above, and R is hydrogen, a hydroxyl group or a structure of the formula V, R is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V and R and R are as defined above, is reacted with (R)- or (S)-glycidyl sulphonate.