发明名称 CAMPTOTHECIN DERIVATIVES AND PROCESS FOR PREPARING SAME
摘要 <p>New Camptothecin derivatives possessing high anti-tumor activity with slight toxicity, represented by the general formula: wherein R1 stands for a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group, R2 for a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, a carboxymethyl group or an acyloxymethyl group, and R3 for the grouping -XR' (where R' is a hydrogen atom, an alkyl group or an acyl group and X is an oxygen atom or a sulfur atom), a nitro group, an amino group, an alkylamino group, an acylamino group or a halogen atom, with the proviso that when both of R1 and R2 are hydrogen atoms, R3 should not be hydroxyl group, methoxy group or acetoxy group. These new camptothecin derivatives are prepared by treating a 5-R1-7-R2-camptothecin derivative with a peroxidant and then reacting the resultant 5-R1-7-R2-camptothe-cin-1-oxide with an active hydrogen compound under irradiation of UV-rays or by catalytically hydrogenating the ring B of camptothecin in a solvent, treating the resultant tetrahydro product with an acylating agent, introducing nitro group into 10-position of the acylated product by the reaction with nitric acid, splitting off the acyl group in the 10-nitro product by hydrolysis and treating the hydrolyzed tetrahydro product with an oxidizing agent for dehydrogenation, and if desired, reducing the nitro group in the resultant product to amino group and modifying the amino group by N-alkylation, N-acylation or by diazotization followed by hydrolysis or Sandmeyer reaction, before or after the oxidation of the 10-nitro-tetrahydro product. - 1a</p>
申请公布号 CA1246576(A) 申请公布日期 1988.12.13
申请号 CA19820410691 申请日期 1982.09.02
申请人 KABUSHIKI KAISHA YAKULT HONSHA 发明人 MIYASAKA, TADASHI;SAWADA, SEIGO;NOKATA, KENICHIRO;MUTAI, MASAHIKO
分类号 C07D491/22;(IPC1-7):C07D491/22 主分类号 C07D491/22
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