Patent ID: 6218519
Filing Date: 2001-04-17
Classification: C07H

Abstract:
A compound of the formula ##STR4##where:R.sup.1 is a radical of an anthracyclinone where the point of attachment is the 3' nitrogen of the daunosamine sugar;R.sup.2 is H, alkyl having from 1 to 6 carbon atoms, aromatic having from 6 to 10 carbon atoms or heteroaromatic having from 5 to 8 atoms in the heteroaromatic ring substituted with NO.sub.2, CN, F, Cl, OH, alkoxy having from 1 to 6 carbon atoms, COMe, CF.sub.3, COOH, COO alkyl having from 1 to 10 carbon atoms or COO aryl having from 6 to 10 carbon atoms;R.sup.3 is cyano, methoxy, ethoxy, alkoxy having from 3 to 18 carbon atoms, or aryloxy having from 6 to 10 carbon atoms substituted with NO.sub.2, CN, F, Cl, OH, alkoxy having from 1 to 6 carbon atoms, COMe, CF.sub.3, COOH, or COO alkyl having from 1 to 10 carbon atoms or COO aryl having from 6 to 10 carbon atoms, acetoxy, propionyloxy, trimethylacetoxy, or benzoyloxy;X=CH.sub.2, O, S, or N substituted by H, alkyl or acyl having from 1 to 6 carbon atoms, aromatic having from 6 to 10 carbon atoms or heteroaromatic having from 5 to 8 carbon atoms in the heteroaromatic ring substituted with methyl, ethyl, acetyl or benzoyl;n=2 if X=O, S, or substituted N;n=1 or 2 if X=CH.sub.2 ;B is O, NHCOO, or one of the following substituted aromatics: ##STR5##wherein from 1-4 Ms are substituted on the ring and where M is H, NO.sub.2, CN, F, Cl, OH, alkoxy having from 1 to 18 carbon atoms in the heteroaromatic ring, COMe, CF.sub.3, COOH, COO alkyl having from 1 to 10 carbon atoms or COO aryl having from 6 to 10 carbon atoms, aromatic having from 6 to 10 carbon atoms or heteroaromatic having from 5 to 8 atoms in the heteroaromatic ring, methyl or alkyl having from 2 to 18 carbon atoms; andZ is a glycosyl, or substituted aliphatic acyl having from 1 to 18 carbon atoms or aromatic acyl having from 6-10 carbon atoms, attached to the aromatic or carbamoyl O of B at the anomeric carbon of Z;provided that where R.sup.3 is aryloxy, acetoxy, propionyloxy, trimethylacetoxy, or benzoyloxy, BZ cannot be the same as R.sup.3.