|
| 摘要: |
| 目的合成标题化合物，并进行工艺改进。方法以1-乙酰基-2,3,5三-O-苯甲酰基-β-D-呋喃核糖为起始原料，制得1-氯-2-脱氧-2-氟-3,5-二-O-苯甲酰基-α-D-阿拉伯糖(化合物6）。化合物6与2-氯腺嘌呤在四氯化锡作用下发生缩合反应生成氯法拉滨。结果总收率为8.4%，目标化合物的结构经IR、1H-NMR、MS等方法确证。结论该合成工艺具有原料易得，操作简便，易于工业化生产等特点。 |
| 关键词: 工艺改进 化学合成 氯法拉滨 抗白血病 |
| DOI： |
| 分类号: |
| 基金项目: |
|
| Improved Synthesis of Clofarabine |
|
GUO Shunmin，DENG Sishan，QI Yiping，LIN Sui
|
| Abstract: |
| OBJECTIVE To synthesize the title compound and improve the process. METHODS 3,5-di-O-benzoyl-2-deoxy-2-fluoro-α-D-arabinofuranosyl chloride (compound6) was synthesizes from 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose.clofarabine was obtained by the reaction of the compound 6 and 2-chloroadenine in the presence of SnCl4. RESULTS The total yield was up to 8.4%.The target compound was identified by IR，1H-NMR and MS. CONCLUSION The improved process is simple and easy for a scale production. |
| Key words: process improvement chemical synthesis clofarabine antileukemie |
