Antitumor glycosides, their preparation, use and...

C - Chemistry – Metallurgy – 07 – H

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260/208.2

C07H 15/24 (2006.01) C07H 13/08 (2006.01) C07H 15/252 (2006.01)

Patent

CA 1154013

ABSTRACT OF THE DISCLOSURE Anthracycline glycosides of the formula I Image I wherein R is hydrogen or hydroxy, one of R1 and R2 is methyl and the other of R1 and R2 is hydroxy, and pharmaceutically accept- able acid addition salts thereof, which are useful in treating certain mammalian turmors, are prepared by condensing daunomy- cinone 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.

359119

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