摘要
以胸苷为原料,6位醇羟基用对甲氧基苯甲酸成酯保护,然后与偶氮二甲酸二乙酯和三苯基瞵反应成"氧桥",再与叠氮化钠反应上"叠氮",最后在绿色介质离子液体中脱保护得齐多夫定,收率76%。该工艺反应条件温和、原料易得、操作简便、产率高、环境友好,既适应于工业化生产,又使成本显著降低,且反应介质离子液体可方便回收并重复利用。
Zidovudine was synthesized in ionic liquids from thymi- dine. Thymidine was esterified with 4-methoxybenzoic acid to protect its primary alcoholic hydroxyl at 6 position and then was converted into 2, 3＇-anhydro-5＇- O-（4-methoxybenzoyl） thymidinc via the reaction with diethyl azodiearboxylatc and triphenylphosphine .3 was treated with sodium azide to form 3＇-azido-3＇-deoxy- 5＇- O-（4-methoxybenzoyl） thymidine, followed by 5＇- O-deprotection to yield 1 at an overall yield of 76 % . The method is simple and suitable for commercialization. The method presented hereby features mild reaction conditions, simple operation, readiness for product isolation, high yield, and environmental benignity. Furthermore, the ionic liquid can be easily recycled and reused for several runs efficiently.
出处
《化学试剂》
CAS
CSCD
北大核心
2009年第1期23-24,30,共3页
Chemical Reagents
