摘要 |
NEW MATERIAL:A compound of formula I (R1 is H, methoxy; R2, R3 are H, hydroxyl; R4 is hydroxyl, when R<3> is H, or H, when R<3> is hydroxyl; X is divalent organic group; Y is the residue of the alcohol in activated ester). EXAMPLE:N-[4-(N-Succinimidyloxy) carbonylbutyryl] acetyldaunomycin. USE:A synthetic intermediate of a carcinostatic agent. PREPARATION:The esterification of a carboxylic acid of formula II gives a compound of formula I. The carboxylic acid of formula II as a a starting substance is obtained by allowing an anthracyclin of formula I with a haloacetyl N-succinimidyl ester of formula IV (Z is C1, Br, I), then allowing a monosodium salt of a dibasic acid of formula VI to act on the resultant alpha-halocarbonyl derivative of formula V.
|