METHOD OF MAKING THE NEW 4-SUBSTITUTED DERIVATIVES OF DAUNORUBICINE

Compounds of the formula: wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl or benzyl; A and B are OH or A and B are OCOOR4 or B is OH and A is OCOOR4; and R4 is alkyl which are intermediates for the preparation of antitumor compounds of the formula: I wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl;...

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Hauptverfasser: MASI,PAOLO,IT, ARCAMONE,FEDERICO,IT, BERNARDI,LUIGI,IT, SUARATO,ANTONINO,IT
Format: Patent
Sprache:eng
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Zusammenfassung:Compounds of the formula: wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl or benzyl; A and B are OH or A and B are OCOOR4 or B is OH and A is OCOOR4; and R4 is alkyl which are intermediates for the preparation of antitumor compounds of the formula: I wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl; a C3-C6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X-Phe-(CH2)n-, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R2 is hydrogen, hydroxyl or acyloxy (R-COO-); where R is an alkyl having from 1 to 11 carbon atoms; and R3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids.