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.
出处
《合成化学》
CAS
CSCD
2002年第5期405-408,共4页
Chinese Journal of Synthetic Chemistry
