发明名称 ANTHRACYCLIN DEIVATIAVE AND ITS PREPARATION
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.
申请公布号 JPS61129194(A) 申请公布日期 1986.06.17
申请号 JP19840249791 申请日期 1984.11.28
申请人 TEIJIN LTD 发明人 KATO YOSHINORI;HARA TAKESHI
分类号 C07H15/252;A61K31/70;A61K31/7028;A61K31/7034;A61K31/704;A61P35/00 主分类号 C07H15/252
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