抗白血病药物氟达拉滨的简便合成  

THE NEW SYNTHESIS OF ANTI-LEUKEMIA DRUG FLUDARABINE

作　　者：夏然[1] 孙莉萍[2] 杨西宁 渠桂荣[4] 

机构地区：[1]新乡学院化学化工学院,河南新乡453003 [2]新乡学院生命科学与技术学院,河南新乡453003 [3]新乡拓新生化股份有限公司,河南新乡453003 [4]河南师范大学化学化工学院,河南新乡453007

出　　处：《精细石油化工》2016年第1期30-33,共4页Speciality Petrochemicals

基　　金：国家自然科学基金(21172059);新乡学院科技创新基金重点培养项目(15ZP06)

摘　　要：以2-氨基阿糖腺苷为原料,以吡啶·HF/NaNO_2为氟代试剂,在室温条件下搅拌反应10h,可以选择性地将嘌呤2位—NH_2转化为—F,一步得到氟达拉滨,收率81%。考察了氟代试剂、原料配比、温度、时间及反应规模对收率的影响。该方法避免了官能团保护和脱保护的繁琐步骤,不使用重金属催化剂,且反应规模扩大至1kg时,收率达到80%。A new method for the synthesis of fludarabine was developed.Fludarabine was obtained in one step and 81% yield from 2-aminoadenosine at room temperature for 10 hby transforming amino group to fluoride using pyridine·HF and NaNO_2 as fluorination regents.The effects of fluorinationregents,substrate ratios,reaction temperature,reaction time and reaction scale on the yields were investigated.The presented method avoided the tedious group protection and deprotetion steps,and did not need toxic metal catalysts.Moreover,fludarabine was afforded successfully in 80% yield even on a 1kg scale.

关 键 词：氟达拉滨 2-氨基阿糖腺苷 合成方法 氟代 

分 类 号：TQ463.5[化学工程—制药化工]