Anthracycline glycosides, their preparation, use and composition

Details Anthracycline glycosides, their preparation, use and composition Anthracycline glycosides, their preparation, use and composition

1980-08-28

1982-04-20

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

435 78, 536 17A, 536 18, 536 53, 424181, A61K 3171, C07H 1522, C07H 1524

Patent

active

043259464

ABSTRACT:
Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxy, one of R.sub.1 and R.sub.2 is methyl and the other of R.sub.1 and R.sub.2 is hydroxy, and pharmaceutically acceptable acid addition salts thereof, which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with certain novel sugars in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form the corresponding protected glycosides from which the protecting groups are removed. This gives the compounds wherein R is hydrogen. The former are converted to the corresponding hydroxyl compounds by treatment with bromine and sodium formate.

REFERENCES:
patent: 3803124 (1974-04-01), Arcamone et al.
patent: 4046878 (1977-09-01), Patelli et al.
patent: 4067969 (1978-01-01), Penco et al.
patent: 4112076 (1978-09-01), Arcamone et al.
patent: 4133877 (1979-01-01), Masi et al.
patent: 4191755 (1980-03-01), Masi et al.
patent: 4265885 (1981-05-01), Bargiotti et al.

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