一种阿糖腺苷合成的新方法

A New Method for Synthesis of Vidarabine

摘要:

阿糖腺苷是一种有效的抗疱疹及带状疱疹病毒药物，也是抗脱氧核糖核酸(DNA)病毒药单磷酸阿糖腺苷以及治疗B-细胞慢性淋巴细胞白血病(B-CLL)特效药氟达拉滨等下游产品合成的主要原料。开发阿糖腺苷的合成方法具有广阔的市场前景。以廉价的腺苷作为原料，经8位溴代、羟基磺酰化、羟基乙酰化、一锅两步完成构型翻转和脱肼等五步反应合成阿糖腺苷是一种新的有效的化学合成法。反应步骤中大多使用自来水作为绿色溶剂，具有工艺简单、安全性高、三废排放少以及经济性高的优势,在工业生产中极具发展潜力。

Abstract:

Vidarabine is well known anti-herpes andanti-herpes zoster virus drugs. It’s also the main raw material for the synthesis of downstream products such as vidarabine monophosphate and fludarabine,which are used as antideoxyribonucleic acid virus drug and B-chronic lymphocytic leukemia(B-CLL) powerful drug. So developing the synthesis of vidarabine has wide foreground on market. Vidarabinewas sffectivelysynthesized through five steps including 8-bromo, hydroxyl-sulfonylation, hydroxyl-acetylationas well as configuration inversions and dehydrazination by “one pot, two steps” methods, stating with adenosine, which can be obtained cheaply and conveniently. This method using water as reaction solvent, has some advantage such as simple craftwork, operate safely, less discharge of the three wastesand aconomic, andwith potential development in industrial production.