| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain epirubicin (salt) useful for antibiotics, etc., in a high purity and in a high yield by subjecting daunomycin (acid adduct) to a methanolysis reaction and further subjecting the product to reactions under specific conditions. SOLUTION: Daunomycin (acid adduct) of formula I is subjected to a methanolysis reaction to obtain a daunomycinone of formula II and daunosamine methyl ether (acid adduct) of formula III. The daunomycinone of formula II is brominated and acetoxylated to produce 14-acetoxydaunomycin of formula IV. A compound of formula V (X is TFA, etc.; Y is OTFA, etc.; Z is a halogen, etc.) obtained from the compound of formula III as a starting raw material is reacted with a compound of formula IV to obtain a compound of formula VI (X is TFA, AIoc), which is protected under a mild basic conditions to obtain a compound of formula VII (R is a 1-4C alkyl). The compound of formula VII is subjected to the removal of trifluoroacetyl group and subsequently to the removal of an acetal-protecting group, and neutralized into epirubicin, which is arbitrarily acidified to obtain epirubicin (salt).</p> |
