文章摘要
路彬,王晓霞,姬鹏燕,魏万磊,金浩,孔凡鹏.一种阿糖腺苷合成的新方法[J].精细化工,2018,35(12):
一种阿糖腺苷合成的新方法
A New Method for Synthesis of Vidarabine
投稿时间:2018-04-08  修订日期:2018-10-22
DOI:
中文关键词: 腺苷  阿糖腺苷  一锅两步  化学合成  抗病毒药物
英文关键词: Adenosine  Vidarabine  one pot, two steps  Chemical synthesis  antiviral drugs
基金项目:甘肃省技术创新引导计划-中小企业创新基金(17CX2JA004)
作者单位E-mail
路彬 兰州奥凯化工公司 517213680@qq.com 
王晓霞 甘肃省化工研究院有限责任公司  
姬鹏燕 甘肃省化工研究院有限责任公司  
魏万磊 甘肃省化工研究院有限责任公司  
金浩 兰州奥凯化工公司  
孔凡鹏 甘肃省化工研究院有限责任公司 908333862@qq.com 
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中文摘要:
      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。
英文摘要:
      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.
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