NOVEL ANTHRACYCLINE DERIVATIVE

摘要

PURPOSE:To provide a novel compound exhibiting a strong antitumor activity. CONSTITUTION:The compound of formula I (R is H, carboxylic acid-protecting group; (n) is 1-7) and its salt, e.g. 3'-N-(3-methoxycarbonyl-1oxopropyl) oxaunomycin. The compound of formula I is obtained by reacting oxaunomycin of formula II with a 1-ethoxyvinyl ester derivative of formula III (R<1> is R) (e.g. l-ethoxyvinyl pivalate) in a halogenated solvent such as dichloromethane under refluxing preferably for 0.25-5hr. The compound of formula II is preferably obtained from the cultured product of Streptomyces D788. PRM-5 strain (FERM P-7703). The compound of formula III is obtained e.g. by reacting a compound of formula IV with ethoxyacetylene in the presence of a ruthenium catalyst.