节点文献
氮杂胞苷的合成工艺研究
Improved synthesis of azacytidine
【摘要】 以氰基胍和甲酸为原料,经成盐、环合反应得到5-氮杂胞嘧啶,5-氮杂胞嘧啶经硅烷化保护后,与乙酰化的核糖成苷,再脱保护基得到氮杂胞苷。目标化合物的结构经1H-NMR、MS谱数据确证,总收率为26.6%。该工艺路线优化了反应条件、简化了操作、提高了收率。
【Abstract】 Cyanoguanidine and acetylated β-D-ribose were used as starting materials to give target compound via salt formation,cyclization,silylation,coupling reaction and deprotection.The target compound was characterized by 1H-NMR,MS spectra and the total yield was 26.6%.The synthetic conditions were optimized and the total yield was increased.
【关键词】 工艺改进;
化学合成;
氮杂胞苷;
氰基胍;
【Key words】 process improvement; chemical synthesis; azacytidine; cyanoguanidine;
【Key words】 process improvement; chemical synthesis; azacytidine; cyanoguanidine;
【基金】 国家自然科学基金海外青年学者合作研究基金项目(30328030)
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2008年05期
- 【分类号】TQ463
- 【被引频次】7
- 【下载频次】385