氮杂胞苷的合成工艺研究  

Improved synthesis of azacytidine

作　　者：郭刚[1] 杨千姣[1] 赵力挥[1] 刘丹[1] 赵临襄[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2008年第5期377-378,383,共3页Chinese Journal of Medicinal Chemistry

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)

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。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 

分 类 号：TQ463[化学工程—制药化工]