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目的改进抗肿瘤药物卡培他滨的合成工艺。方法以5-氟胞嘧啶为原料,经硅醚化后,与5’-脱氧-1’,2’3,’-三-乙酰基-D-核糖缩合,再经酰胺化、水解制得卡培他滨。结果与结论目标化合物的结构经1H-NMR、IR、MS谱确证,总收率为70.0%,改进后的工艺,简化了实验操作,解决了重金属超标问题,有利于工业化生产。
Objective To improve the synthetic capecitabine antitumor drug. Methods 5-fluorocytosine was used as starting material, and after silylation, it was condensed with 5’-deoxy-1 ’, 2’3’-tri-acetyl-D-ribose and then amidated and hydrolyzed to obtain a card Perthihide. Results and Conclusion The structure of the target compound was confirmed by 1H-NMR, IR and MS spectra. The overall yield was 70.0%. The improved process simplified the experimental operation and solved the problem of exceeding the standard of heavy metals, which was benefit to industrialized production.