Process for the preparation of anthracycline derivatives

Details Process for the preparation of anthracycline derivatives Process for the preparation of anthracycline derivatives

C - Chemistry, Metallurgy

07

H

260/208.2

C07H 15/24 (2006.01) C07H 15/252 (2006.01)

Patent

CA 1090787

ABSTRACT OF THE DISCLOSURE Disclosed is a process for the preparation of antitumor compounds of the formula: Image I wherein R1 is a C2-C4 alkyl; a C3-C6 cycloalkyl; a C3-C6 cyclo- alkyl substituted by a halogen, hydroxy, methoxy, amino or di- methylamino 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 pharmaceuticaily acceptable acids. Compounds I are prepared by condensing the aglycones thereof with 2,3,6-trideoxy-3-trifluoro-acetamido-4-O-trifluoro- acetyl-.alpha.-L-lyxopyranosyl chloride according to a conventional technique.

290848

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