卡培他滨的合成工艺研究

Study on the synthesis technology of capecitabine

目的以5-氟胞嘧啶和1,2,3-三-O-5-脱氧-D-呋喃核糖为原料合成抗肿瘤药物卡培他滨,考察制备过程中的各种影响因素,并进行优化。方法以5-氟胞嘧啶为原料,经胺烷基化反应,Silyl缩合反应,酰胺化反应,再经去乙酰基反应得到卡培他滨。结果降低了反应温度,缩短了反应时间,目标产品总收率为73.17%,纯度为99.85%。结论该合成工艺简化了操作,更适合工业化生产。

Objective To synthesize the capecitabine with 5-fluorocytosine and 1,2,3-tri-O-5-deoxy-D-ribofuranosyl as materials,and to investigate the influential factors and optimize the technology conditions.Methods The capecitabine was synthesized from 5-flucytosine and 1,2,3-tri-O-5-deoxy-D-ribofuranosyl through amine alkylation reaction,Silyl condensation reaction,amidation reaction,and then deacetylation reaction.Results The product was obtained with 73.17% yield and 99.85% purity at lower reaction temperature for shorter reaction time.Conclusion The established synthetic technology is simplified,and is more suitable for industrial production.