奈拉滨的合成工艺改进

Improve the Synthetic Method of Nelarabine

目的:改进奈拉滨的合成方法。方法:以2-氨基-6-氯嘌呤和2,3,5-三-O-苄基-1-O-对硝基苯甲酰基-D-阿拉伯呋喃糖为起始原料,经取代、氯代、缩合、水解四步反应合成奈拉滨。结果:合成的目标化合物,其结构经核磁共振氢谱、核磁共振碳谱、质谱及元素分析确证。结论:本方法简化了操作步骤,优化了反应条件,降低了成本,提高了收率。

Objective： To study on synthesis of Ne]arabine by improving method. Method： Nelarabine was synthesized starting from 2-amino-6 -ehloropurine and 2,3,5-Tri-O-bensy]-I -O- （ 4 -nitrobensoy] ） -D-ar-abinofuranose via four steps, including permutation, chlorination, condensation, hydrolysis. Result： The structure of the target compound was confirmed by ＇ H-NMR, 13 C-NMR, MS and ele- mental analysis. Conclusion： This optimal synthetic procedure with lower cost and higher yield is worthy to have a further pilot manu- facture.