| 抗癌药盐酸吉西他滨的合成工艺研究 |
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| 引用本文： | 杨宝海,洪承杰.抗癌药盐酸吉西他滨的合成工艺研究[J].精细与专用化学品,2012,20(2):17-19. |
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| 作者姓名： | 杨宝海 洪承杰 |
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| 作者单位： | 江苏豪森医药研究院有限公司,江苏连云港,222000 |
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| 摘 要： | S-甘油醛缩丙酮经Reformasty反应、脱异丙叉基保护、内酯化及双苯甲酰化得到2-脱氧-2,2-二氟-D-赤型-呋喃戊糖-1-酮-3,5-二苯甲酸酯,再经四氢铝锂还原、甲磺酰化、缩合得2-脱氧-2＇,2＇-二氟胞苷-3＇,5＇-二苯甲酸酯,然后经脱保护基,成盐后经丙酮-水体系重结晶分离得盐酸吉西他滨,总收率6.2%。
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| 关 键 词： | 盐酸吉西他滨 S-甘油醛缩丙酮 抗肿瘤药 合成 |
Synthesis of gemcitabine hydrochloride |
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| YANG Bao-hai,HONG Cheng-jie.Synthesis of gemcitabine hydrochloride[J].Fine and Specialty Chemicals,2012,20(2):17-19. |
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| Authors: | YANG Bao-hai HONG Cheng-jie |
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| Affiliation: | (Jiangsu Hansoh Medicine Insititute Co.,Ltd.,Lianyungang 222000,China) |
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| Abstract: | 3,5-Di-O-benzoyl-2-deoxy-2,2-difluoro-D-ribose was prepared from （S）-glyceraldehyde acetonide via successively Reformasty reaction, deprotect, lactonization and benzoylation. The resulting intermediate was converted to 2 ＇-deoxy-2 ＇ , 2 ＇-difluoro-3 ＇ , 5 ＇-di-O-benzoyl-cytidine via reduction with LiA1H4, methylsulfonation and condensation. Then protect group was removed and the crude product salt was obtained in HC1. After a crystallization in aqueous acetone, the final product was got with an overall yield of 6.2%. |
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| Keywords: | gemcitabine hydrochloride （S）-glyceraldehyde acetonide antitumor drug synthesis |
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