卡培他滨的合成工艺改进

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。

Improved synthesis of capecitabine

Capecitabine,an antitumor agent,has been used for the treatment of breast cancer or rectal cancer caused by cancer cell.To improve the synthetic procedure of capecitabine,a confluent synthetic route was designed and used to prepare the target compound in this paper.The target compound,capecitabine,was facilely synthesized from 5-fluorocytosine by silylation with hexamethyldisilazane,condensation with 1,2,3-tri-O-acetyl-5-deoxy-β-D-ribose to give 2′,3′-di-O-acetyl-5′-deoxy-5-fluorocytidine,followed by amidation with n-pentyl chloroformate,and then hydrolysis with an overall yield of about 70%.The structure of capecitabine was confirmed by 1H-NMR,IR,MS.In this improve procedure,the key intermediate 4,2′,3′-di-O-acetyl-5′-deoxy-5-fluorocytidine,was easy to extract by changing the catalyst for condensation.And then the target compound was synthesized by one-step-one pot.The improved process is easy for synthesis and suitable for industrial manufacturing,and able to solve the problem of heavy metals exceeding. capecitabine