盐酸阿糖胞苷和盐酸环胞苷工艺研究  

Study on the Synthesis of Cytarabine Hydrochloride and its Intermediate Ancitabine Hydrochloride

作　　者：饶哲[1] 张珩[1] 杨艺虹[1] 张秀兰[1] 王贝[1] 

机构地区：[1]武汉工程大学绿色化工过程省部共建教育部重点实验室,湖北武汉430073

出　　处：《精细化工中间体》2013年第6期29-32,共4页Fine Chemical Intermediates

基　　金：武汉工程大学研究生教育创新基金(CX201212)

摘　　要：以胞苷为原料,经过缩合、水解反应合成2种抗白血病药物盐酸环胞苷(中间体)及盐酸阿糖胞苷。采用正交实验法,对缩合反应中原料与催化剂的配比、原料的浓度、反应温度等因素进行了工艺优化。通过IR、GC-MS、1H NMR确证了盐酸环胞苷及盐酸阿糖胞苷的结构。该合成路线工艺简单、原料易得、条件温和、操作简便,总收率达32.2%,具有工业化应用价值。Ancitabine hydrochloride and its derivative cytarabine hydrochloride are important antileukemia drugs. Both compounds were synthesized starting from cytidine and reaction conditions were optimized. The overall yield of cytarabine hydrochloride was 32.2%,and the chemical structure was identified with IR, GC-MS and 1H NMR spectra. The synthetic process is simple, convenient and easy to operate in industrial scale.

关 键 词：抗白血病药物 盐酸环胞苷 盐酸阿糖胞苷 正交实验法 合成 

分 类 号：TQ464.3[化学工程—制药化工]