ANTHRACYCLIN-GLYCOSIDE, VERFAHREN ZU IHRER HERSTELLUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNG
Anthracycline glycosides of the formula I 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 acceptable acid addition salts thereof, which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone...
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Zusammenfassung: | Anthracycline glycosides of the formula I 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 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. |
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