8-氯腺苷衍生物的合成及生物活性研究  

Synthesis and Biological Activities of 8-Cl-Adenosine Derivatives

作　　者：林桂椿[1] 刘莉[1] 张亮仁[1] 张礼和[1] 

机构地区：[1]北京大学药学院天然药物及仿生药物国家重点实验室,北京100083

出　　处：《合成化学》2002年第5期405-408,共4页Chinese Journal of Synthetic Chemistry

摘　　要：N6-甲基 -8-氯腺苷的合成是以 N ,N -二甲基乙酰胺为溶剂由腺苷与碘甲烷反应 ,生成 N1-甲基 -8-氯腺苷 ,经过 Dimorth重排而得到 ,优化反应条件后 ,N1-甲基 -8-氯腺苷收率为 5 2 %。8-氯腺苷糖环羟基被酯化后失去原有的生物活性 。For improving the bio-availability of 8-chloro-adenosine, its derivatives were synthesized, in which N 6-methyl-8-chloro-adenosine was synthesized via Dimorth rearrangement reaction. Anti- tumor activity assay showed that the activity was maintained after the 6-NH 2 was methylated, whereas, the activity was lost after the hydroxyl groups of ribose were esterified.

关 键 词：8-氯腺苷衍生物 合成 生物活性 Dimorth重排 N^6-甲基-8-氯腺苷 抗肿瘤药物 核苷类药物 

分 类 号：TQ464.6[化学工程—制药化工] R979[医药卫生—药品]