Antitumor glycosides, their preparation and use

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 17A, A61K 3170, C07H 1524

Patent

active

042762898

ABSTRACT:
Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.

REFERENCES:
patent: 4046878 (1977-09-01), Patelli et al.
patent: 4077988 (1978-03-01), Arcamone et al.
patent: 4107423 (1978-08-01), Arcamone et al.
patent: 4183919 (1980-01-01), Cassinelle et al.

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