抗癌药物盐酸吉西他滨的合成  

Synthesis of anti-tumor drug gemcitabine hydrochloride

作　　者：顾秀娟[1] 赵敏[1] 吴范宏[1] 赛达力木[1] 

机构地区：[1]华东理工大学,上海200237

出　　处：《中国新药杂志》2010年第16期1463-1464,共2页Chinese Journal of New Drugs

摘　　要：目的:合成抗癌药物盐酸吉西他滨并改进合成工艺。方法:以2-脱氧-2,2-二氟-D-赤型-呋喃戊糖-3,5-二苯甲酸酯-1-甲磺酸酯为原料,经与碱基缩合,脱羟基保护基,成盐,异构体分离得盐酸吉西他滨。结果:合成了盐酸吉西他滨,总收率15.8%。结论:本方法具有可行性。Objective： To synthesize of gemcitabine hydrochloride and optimize the process.Methods： Gemcitabine hydrochloride was prepared from 2-deoxy-2,2-difluoro-D-ribofuranose-3,5-dibenzoate-1-methylsulfonate,by condensation with cytosine followed by deprotection,salt formation and crystallization in aqueous acetone.Results： Gemcitabine hydrochloride was synthesized.The total yield of gemcitabine was 15.8%.Conclusion： This synthetic method was feasible.

关 键 词：盐酸吉西他滨 抗癌药物 碘化钾 催化 合成 

分 类 号：R979.1[医药卫生—药品]