【摘要】 目的:改进已有的以2′,3′,5′-三-氧-乙酰基鸟苷为原料合成药物中间体2-氨基-6-氯-9-β-D-呋喃核糖基嘌呤的方法。方法:对鸟苷6-羟基的氯置换反应过程作了较多改进:(1)去除影响产品质量的原辅材料N,N-二甲基苯胺;(2)用混合溶剂乙腈-二氯乙烷代替单一溶剂无水乙腈;(3)以三光气代替三氯氧磷作为氯化剂。结果与结论:经过方法(1)和(2)的改进,简化了氯置换反应过程与操作,减少了副反应,使反应收率有所提高;方法(3)可免除磷污染。更多还原

【Abstract】 Objective:To improve the method for synthesis of 2-amino-6-chloro-9-β-D- ribofuranosylpurine starting from 2′,3′,5′-tri-O-acetylguanosine. Methods:In the chlorodisplacement reaction of 6-hydroxy group in guanosine, N,N-dimethylaniline which influenced the quality of product was discarded , the mixed solvent acetonitrile-dichloroethane was used and phosphoryl chloride which was used as chlorinating agent was replaced by triphosgene. Results and Conclusion:The procedure of chlorodisplacement was simplified, side-reaction was reduced, and the yield of product was increased. Apart from this, the phosphorus pollution can be avoided through the replacement of phosphoryl chloride by triphosgene.更多还原