卡培他宾的合成工艺研究  

Synthetic technology of capecitabine

作　　者：刘杨[1] 骆伟[1] 孙厉[1] 陶然[1] 郭春[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2009年第2期120-122,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的合成抗肿瘤药卡培他宾。方法以D-核糖为起始原料,通过缩醛保护、对甲苯磺酰化、溴代、氢化脱卤、脱保护和乙酰化共6步反应制得中间体5-去氧-1,2,3-三-O-乙酰基-D-核糖(7),N4-正戊氧羰基-5-氟胞嘧啶与7进行缩合后,再经氨解脱乙酰基得到目标化合物。结果与结论目标化合物的总收率为16.4%(以D-核糖计),其结构经1H-NMR、MS确证。该合成工艺简化了操作,降低了合成成本,适于工业化生产。Aim To synthesize anticancer agent capecitabine. Methods 5-Deoxy-1,2,3-tri-O-acetyl-D-ribo- furanoside （7） was prepared from D-ribofuranoside through 6 steps like protection, sulfonylation, bromation, reduction,deprotection and acetylation. Then compound 7 was condensed with 5-fluoro-N^4-（ pentyloxycarbonyl） cytosine and capecitabine was obtained followed by deprotection. Results and conclusion The structure of capecitabine was confirmed by ^1H-NMR spectrum and MS. The total yield of the process is 16.4% （ based on D-ribofuranoside）. This synthetic process is applicable in industrial preparation with a lower cost and simplified operation.

关 键 词：卡培他宾 合成工艺 抗癌 

分 类 号：TQ463.53[化学工程—制药化工]