| 摘要 |
An improved process for the production of anthracycline derivatives of the general formula;
<CHEM>
wherein R<2> is hydrogen, tetrahydropyranyl, 6-acetoxymethyltetrahydropyranyl, 6-methoxytetrahydropyranyl, 6-carbomethoxytetrahydropyranyl, tetrahydrofuranyl, 1-methoxyethyl, 1-ethoxyethyl, 1-butyloxyethyl, 1-isobutyloxyethyl, 1-(6-methylheptyloxy) ethyl or cyclohexyloxyethyl group, which comprises reacting 14-halogenodaunomycin of the formula;
<CHEM>
wherein X is halogen atom; or a salt thereof, with dihydropyrane, 2-acetoxymethyl-3,4-dihydro-2H-pyrane, 2-methoxy-3,4-dihydro-2H-pyrane, 2-carbomethoxy-3, 4-dihydro-2H-pyrane, dihydrofurane, methylvinylether, ethylvinylether, butylvinylether, isobutylvinylether, 6-methylheptylvinylether or cyclohexylvinylether, in the presence of an acid catalyst in an organic solvent, hereby obtaining 14-halogenodaunomycin derivatives of the formula;
<CHEM>
wherein R<2>, X have the same meaning as defined above except for hydrogen,
and treating with an alkali 14-halogenodaunomycin or the 14-halogenodaunomycin derivatives obtained in the preceding step, in a lower alcohol or aqueous acetone to effect hydrolysis, hereby obtaining anthracycline glycosides of the formula;
<CHEM>
wherein R<2> has the same meaning as defined above, or an acid salt thereof. |
