发明名称 CORIOLIN DERIVATIVE AND ITS PREPARATION
摘要 NEW MATERIAL:A compound of formula I: (one of X and Y is group of formula II, and the other is >C-OH, >C=O, or the group of formula II. EXAMPLE:1alpha-Octanoyl-4beta,15: 6beta,7beta-dioxide-5beta-hydroxy-8(22-methylene-21-butanolide) hirsutan. USE:Carcinostatics having life prolongation effects on mouse leukemia L-1210, improved inhibitory activities against experimental tumor cells, e.g. HeLa cells, compared with the well-known coriolin compounds, and expected remedy effects on human tumors. PROCESS:A compound of formula III: (one of X' and Y' is =O, and the other is =O or -OH) is reacted with an alpha-halogenomethylacrylate, e.g. methyl alpha-bromomethylacrylate, in the presence of a metallic zinc, in a solvent, e.g. THF, at room temperature-100 deg.C for 20min-24hr to give the objective compound of formula I.
申请公布号 JPS54154755(A) 申请公布日期 1979.12.06
申请号 JP19780063321 申请日期 1978.05.29
申请人 NIPPON KAYAKU KK 发明人 NAKAYAMA TAKEYA;KUNISHIMA AOI;MATSUDA AKIRA;TAKEUCHI TOMIO
分类号 A61K31/365;A61P31/04;A61P35/00;A61P35/02;C07D493/20;C07D493/22 主分类号 A61K31/365
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