四苄基阿糖胞苷的合成  

Synthesis of Tetrabenzyl Cytarabine

作　　者：梁爽[1] 刘家安[1] 冯德日 王妍妍[1] 辛海龙[1] 许佑君[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]沈阳医学院,辽宁沈阳110034

出　　处：《辽宁化工》2013年第11期1271-1273,共3页Liaoning Chemical Industry

摘　　要：通过选用三苯甲基选择性保护阿拉伯糖5'-位羟基、苄基保护4-位氨基和2',3'-位羟基,于酸性条件下选择性脱除三苯甲基合成了制备阿糖胞苷5'-位氨基酸酯类前药的关键中间体—四苄基阿糖胞苷,苄基保护基可经催化氢化顺利脱除。各步反应条件温和,收率高,操作简便。By using triphenylmethyl to protect 5＇-OH and benzyl to protect 4-NH2 and 2＇, 3＇-di OH of cytarabine, tetra-benzyl cytarabine, the key intermediate of 5＇-amino acid ester derivatives of cytarabine prodrug, was synthesized. Then, the benzyl groups were removed by hydrogenation. Each reaction condition was mild and yield was high as well.

关 键 词：阿糖胞苷 选择性保护 三苯甲基 苄基 

分 类 号：TQ463[化学工程—制药化工]