文献类型：期刊文献

中文题名：卡培他滨的合成

英文题名：Synthesis of capecitabine

作者：党晓翠[1];赛达力木[1];赵敏[1];方向[1];杨雪艳[1]

机构：[1]华东理工大学化学与分子工程学院,上海200237

年份：2013

卷号：22

期号：8

起止页码：967

中文期刊名：中国新药杂志

外文期刊名：Chinese Journal of New Drugs

收录：CSTPCD;;Scopus;北大核心:【北大核心2011】；CSCD:【CSCD_E2013_2014】；

基金：上海市联盟计划(LM2010250)

语种：中文

中文关键词：D-核糖;卡培他滨;抗癌药;工艺改进

外文关键词：D-ribose ; capecitabine ; antitumor drug ; process improvement

摘要：目的:合成抗肿瘤药物卡培他滨。方法:以D-核糖为原料,经缩酮化、酯化、还原、水解、乙酰化反应制得1,2,3-三-O-乙酰基-5-脱氧-6-呋喃核糖(7),7与硅醚化的5-氟胞嘧啶缩合制备了2',3'-O-二乙酰基-5'-脱氧-5'-氟胞苷(8),8再与氯甲酸正戊酯反应得到2',3'-O-二乙酰基-5'-脱氧-5-氟-N4-[(戊氧基)羰基]胞苷(9),9经皂化合成卡培他滨。结果:合成了抗肿瘤药物卡培他滨,总收率为25.0%。结论:本方法提高了卡培他滨的反应收率,简化了操作,适合工业化生产。
Objective ： To synthesize the antitumor drug capecitabine. Methods ： D-ribose was taken as the starting material. After ketalization, esterification reduction, hydrolysis and acylation, 1,2,3-tri-O-acetyl-5-deoxy- 13-3-D-ribose （7） was obtained. The condensation of compound 7 and hexamethyl disilylamine 5-fluorocytosine pro- duced 2＇,3＇-O-diacetyl-5＇-deoxy-5-flurocytosine （8）, then compound 8 reacted with n-pentyl chloroformate to get compound 9, eventually the desired product capecitabine was obtained after the saponification of compound 9. Re- suit： The antitumor drug capecitabine was successfully synthesized with a total yield of 25.0%. Conclusion： This method for the synthesis of capecitabine offers high yield by simple operation process, which is suitable for industri- al production.