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US 4,393,052 AGranted
Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsAlberto Bargiotti, Giuseppe Cassinelli, Sergio Penco, Federico Arcamone, Annamaria Casazza
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Abstract
Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-threo-hexopyranosy l chloride; 2,3,4,6-tetradeoxy-4-C-methylene-3-trifluoroacetamido-L-arabino-hexopyrano syl chloride or 2,3,6-trideoxy-4-C-trifluoroacetamidomethyl-3-trifluoroacetamido-3-O-trifl uoroacetyl-L-lyxo-hexopyranosyl chloride.
Claims10
An anthracycline glycoside of the formula I:
- ##STR5## wherein R.sub.1 is hydrogen or hydroxy;
- R.sub.2 is hydrogen or trifluoroacetyl;
- R.sub.3 is methyl, hydroxymethyl, aminomethyl or trifluoroacetylaminomethyl;
- and R.sub.4 is hydrogen or hydroxy, with the proviso that when R.sub.4 is hydroxy, R.sub.3 is aminomethyl;
- or R.sub.3 and R.sub.4 together form methylene, and pharmaceutically acceptable acid addition salts thereof.
2 more elements
A sugar compound selected from the group consisting of ##STR6##
Dependencies are inferred from the claim text.