Anthracycline derivatives, their preparation and use

Details Anthracycline derivatives, their preparation and use Anthracycline derivatives, their preparation and use

1979-01-08

1982-04-27

Hines, Robert V.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

C07C 3940

Patent

active

043270298

ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl or benzyl; A and B are OH or A and B are OCOOR.sub.4 or B is OH and A is OCOOR.sub.4 ; and R.sub.4 is alkyl which are intermediates for the preparation of antitumor compounds of the formula: ##STR2## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl; a C.sub.3 -C.sub.6 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--(CH.sub.2).sub.n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R.sub.2 is hydrogen, hydroxyl or acyloxy (R--COO--); where R is an alkyl having from 1 to 11 carbon atoms; and R.sub.3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids.

REFERENCES:
patent: 3074975 (1963-01-01), McCormic et al.
patent: 3201424 (1965-08-01), McCormic et al.
patent: 3803124 (1974-04-01), Arcamone et al.

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