一种解决卡培他滨重金属超标问题的合成工艺

A solution to the problem Capecitabine synthesis of heavy metals exceeding

目的:改进抗肿瘤药物卡培他滨中间体产物5'-脱氧-2',3'-O-二乙酰-5-氟胞苷的合成工艺,解决生产遇到的成品重金属不合格问题,方法:5'-脱氧-2',3'-O-二乙酰-5-氟胞苷制备过程中,分别考察了用碳酸氢钠固体、2mol/L氢氧化钠溶液、碳酸钠固体中和反应液对后处理操作及产品质量的影响。结果:用碳酸钠固体中和反应液为最佳合成工艺。结论:改进后的合成工艺,简化了生产操作,解决成品重金属不合格问题。

Objective：To improve the synthetic of 5＇-deoxy-2＇,3＇-O-acetyl-5-fluorocytosine,to solve the production problems encourtered in the finished metal failure.Methods：In the preparation process of 5＇-deoxy-2＇,3＇-O-acetyl-5fluorocytosine,the effect of NaHCO3,Na2CO3,NaOH on the simply extent of operation and the yield of product was studied.Results：The optimum reaction condition was that Na2CO3 neutralize in the reactoin solution.Conclusion：The improved synthesis process,streamlining the production poeration,failure to solve the problem of heavy metals finished produce.