C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 15/252 (2006.01) A61K 31/65 (2006.01) A61K 31/70 (2006.01) C07C 50/36 (2006.01) C07C 50/38 (2006.01) C07C 69/757 (2006.01) C07H 15/26 (2006.01)
Patent
CA 2055334
BEHRINGWERKE AKTIENGESELLSCHAFT 90/B 033 - Ma 863 Dr. Ha/Sd Abstract of the disclosure: Semisynthetic diastereomerically pure N-glycidylanthra- cyclines, a process for the stereoselective preparation thereof and the use thereof as cytostatics The invention relates to anthracyclines having cytostatic activity and the formula I, which are, where appropriate, in the form of a salt with an inorganic or organic acid, I Image in which R1 is hydrogen or a hydroxyl group, R2 is hydrogen, a hydroxyl group or an alkyloxy group (C1-C4), R3 is hydrogen, a hydroxyl group or a structure of the formula II II Image R4 is CH2CH3, COCH3, COCH2OH, CHOHCH3 or CHOHCH2OH, R5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II, R5 is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group, a tetrahydropyranyl group, - 2 - R7 is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or di-methyloxy-substituted benzyl group and R6 is a structure of the formula III or IV III Image IV Image and to a process for the preparation of these compounds, which comprises reacting an anthracycline derivative of the structure I in which R1, R2 and R4 are as defined above, and R3 is hydrogen, a hydroxyl group or a structure of the formula V V Image R5 is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V and R6 and R7 are as defined above, with (R)- or (S)-glycidyl sulfonate.
Gerken Manfred
Grimm Monika
Hoffmann Dieter
Raab Ernst
Straub Reiner
Behringwerke Aktiengesellschaft
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
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