抗癌药物盐酸吉西他滨的合成

Synthesis of anti-tumor drug gemcitabine hydrochloride

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.