BIOLOGICALLY-ACTIVE POLYMER-BOUND ANTHRACYCLINES, INTERMEDIATES, PREPARATION METHODS, AND PHARMACEUTICAL COMPOSITION Russian patent published in 2000 - IPC

FIELD: preparation of biologically-active compounds. SUBSTANCE: invention provides new soluble synthetic polymer-bound anthracyclines manifesting antitumor activity. Polymer-bound anthracycline with general formula A (presented in description) is prepared via interaction of polymeric intermediate of formula B: (B), wherein n = 0 or 1, x = 70- 98 mol %, w = 30 to 2 mol %, R₁ is 2-hydroxypropyl or 2-hydroxyethyl; R₂ is 2,4-dichlorophenoxy, p-nitrophenoxy group or hydroxyl, with anthracycline derivative of general formula H-Y-[NH-D], wherein [NH- D] is residue of anthracyclinaminoglycoside having general formula Q: (Q), wherein one of R' and R'' is hydrogen atom and the other hydroxyl or iodine, R''' is hydrogen or methoxy group, R^IV hydrogen or hydroxyl; Y is peptide moiety selected from group including Gly-Phe- Gly, Gly-Leu-Gly, Phe-Leu-Gly, Gly-Phe-Leu-Gly or Leu-Leu-Gly (if R^IV is hydrohyl), in presence of N-ethoxycarbamoyl-2-ethoxy-1,2- dihydroquinoline. If necessary, polymer-bound anthracycline is treated with hydroxypropylamine. Reaction is carried out in anhydrous polar solvent at 15 to 30 C for 8 to 24 h. Polymer-bound anthracycline thus obtained has average molecular weight 29800-33400 and polydispersity 1.4-1.8. EFFECT: extended choice of antitumor drugs. 8 cl, 3 tbl, 18 ex