电化学开环反应合成盐酸阿糖胞苷原料药新工艺  

New Process for Synthesis of Cytarabine Hydrochloride Raw Materials by Electrochemical Ring-opening Reaction

作　　者：陈虎[1] 王献 韩文举 位为晴 李玉生 Chen Hu;Wang Xian;Han Wenju;Wei Weiqing;Li Yusheng(School of Chemical and Pharmaceutical Engineering,Hefei Normal University,Anhui,230601;Anhui Natural Pharmaceutical Co.,Ltd.,Yuekang Pharmaceutical Group,Anhui,236600)

机构地区：[1]合肥师范学院化学与制药工程学院,安徽230601 [2]悦康药业集团安徽天然制药有限公司,安徽236600

出　　处：《当代化工研究》2024年第13期138-140,共3页Modern Chemical Research

基　　金：安徽省科技重大专项项目“抗白血病原料药阿糖胞苷及其系列前药设计与开发”(项目编号:201903a07020003);阜阳市科技重大专项项目“治疗新冠肺炎活性物质穿心莲内酯系列前药设计与开发”(项目编号:FK20208018);安徽高校自然科学研究项目“磷酰化修饰α、β-不饱和酮类GSTπ抑制剂的设计、合成及抗肿瘤活性研究”(项目编号:KJ2020A0088)。

摘　　要：盐酸阿糖胞苷属于抗代谢类的抗肿瘤药物,可掺入肿瘤DNA干扰其复制使细胞死亡,用于各类白血病治疗,是治疗急性淋巴性白血病的首选药物。本文对盐酸阿糖胞苷原料药的合成进行了适合工业化生产的工艺改进,结果表明,经环合和电化学开环反应合成盐酸阿糖胞苷,反应步骤缩短,产率得到了提高,同时减少了有机溶剂等“三废”的排放,降低了生产成本。Cytarabine hydrochloride belongs to the anti-metabolic class of anti-tumor drugs,which can be incorporated into tumor DNA to interfere with its replication and cause cell death.Cytarabine hydrochloride can be used in the treatment of all kinds of leukemia,especially it is the first choice for the treatment of acute lymphoid leukemia.In this paper,the synthesis of cytarabine hydrochloride API is suitable for industrial pro-duction,and it is shown that Cytarabine hydrochloride was synthesized from cytosine nucleoside by cyclization and electrochemical ring-opening re-action.When the yield was increased,the production cost was reduced,the emission of organic solvents and other"three wastes"was reduced.

关 键 词：电化学反应 盐酸阿糖胞苷 工艺改进 盐酸环胞苷 

分 类 号：TQ460[化学工程—制药化工] O621[理学—有机化学]