FORFARANDE FOR FRAMSTELLNING AV DAUNOMYCIN- OCH ADRIAMYCIN-DERIVAT

The novel glycoside antibiotic: 4'-epi-6'-hydroxydaunomycin is prepared by condensing daunomycin with a novel protected, reactive derivative, which is 1,2,3-trideoxy-4,6-di-O-(p-nitrobenzoyl)-3-trifluoroacetamido-L-arabin o-hex-1-enepyranose and thereafter removing the protecting groups. A...

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Bibliographische Detailangaben
Hauptverfasser: A MARCO, A BARGIOTTI, G CASSINELLI, F ARCAMONE
Format: Patent
Sprache:swe
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Zusammenfassung:The novel glycoside antibiotic: 4'-epi-6'-hydroxydaunomycin is prepared by condensing daunomycin with a novel protected, reactive derivative, which is 1,2,3-trideoxy-4,6-di-O-(p-nitrobenzoyl)-3-trifluoroacetamido-L-arabin o-hex-1-enepyranose and thereafter removing the protecting groups. A further novel glycoside antibiotic: 4'-epi-6'-hydroxyadriamycin is prepared by reacting 4'-epi-6'-hydroxydaunomycin with bromine to form an intermediate bromo derivative which is then mildly hydrolyzed to form 4'-epi-6'-hydroxyadriamycin. These novel glycoside antibiotics, while not as effective as the parent compounds daunomycin and adriamycin in the treatment of tumors, are considerably less toxic than the parent compounds.