| 抗癌药物盐酸吉西他滨合成工艺改进 |
| |
| 引用本文： | 徐小娇,杨军,邓鹏飞.抗癌药物盐酸吉西他滨合成工艺改进[J].广东化工,2012,39(1):12-12,21. |
| |
| 作者姓名： | 徐小娇 杨军 邓鹏飞 |
| |
| 作者单位： | 1. 海南师范大学化学与化工学院海南省热带药用植物化学重点实验室,海南海口,571158
2. 上虞颖泰精细化工有限公司,浙江上虞,312369 |
| |
| 摘 要： | 盐酸吉西他滨是一种核苷类抗代谢抗癌药物。笔者利用2-脱氧-2,2-二氟-D-赤型-呋喃戊糖-1-酮-3,5-二苯甲酸酯经四氢锂铝还原,对甲苯磺酰氯酯化,与胞嘧啶缩合,甲醇钠脱保护,成盐后重结晶得盐酸吉西他滨。在对甲苯磺酰氯酯化反应进行改进,改用无水碳酸钾作缚酸剂,降低毒害,经济环保,适合工业化生产。
|
| 关 键 词： | 盐酸吉西他滨 抗癌 合成 |
Improvement of Synthetic Process of the Anti-cancer Drug of Gemcitabine Hydrochloride |
| |
| Xu Xiaojiao,Yang Jun,Deng Pengfei.Improvement of Synthetic Process of the Anti-cancer Drug of Gemcitabine Hydrochloride[J].Guangdong Chemical Industry,2012,39(1):12-12,21. |
| |
| Authors: | Xu Xiaojiao Yang Jun Deng Pengfei |
| |
| Affiliation: | 1.Key Lab of Tropical Pharmaceutical Herb Chemistry of Hainan Province,College of Chemistry and Chemical Engineering,Hainan Normal University,Haikou 571158;2.Shangyu Yingtai Fine Chemical Industry Co.,Ltd.,Shangyu 312369,China) |
| |
| Abstract: | Gemcitabine hydrochloride was an anti-metabolic and anti-cancer nucleoside drug.A method to pro-duce gemcitabine hydrochloride was developed from 2-deoxy-2,2-difluoro-D-erythro-pentofuranose-1-ketose-3,5–di-benzoate via LiAlH4 reduction,p-toluensulfonyl chloride esterification,condensation with cytosine,sodium methox-ide deprotection,salt formation and crystallization.The reaction of p-toluensulfonyl chloride esterification used anh-ydrous potassium.The improvement reduces toxic,and was economic and environmental,suitable for industrial produ-ction. |
| |
| Keywords: | gemcitabine hydrochloride anti-cancer synthesis |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
|
