抗疟药伯氨喹的杂质A及其盐酸盐的合成  

Synthesis of Antimalarial Drug Primaquine Related Compound A and Its Hydrochloride

作　　者：陶乐[1] 李玉江[1] 郭晓河[1] 董黎红[1] 刘陆平 郑果[1] 张方[1] TAO Le;LI Yujiang;GUO Xiaohe;DONG Lihong;LIU Luping;ZHENG Guo;ZHANG Fang(High and New Technology Research Center,Henan Academy of Sciences,Zhengzhou 450002,China)

机构地区：[1]河南省科学院高新技术研究中心

出　　处：《河南科学》2019年第6期887-891,共5页Henan Science

基　　金：河南省科学院人才队伍建设项目(18TP02003,190502003);河南省科学院基本科研费项目(190602008)

摘　　要：以硝基乙烷、丙烯酸甲酯为起始原料,依次进行迈克尔缩合反应、脱甲酯、酰氯化、酰胺化、羰基还原、硝基还原、氨基盐酸盐化等反应,制得抗疟药伯氨喹的杂质A及其盐酸盐,其化学结构经核磁共振氢谱(1HNMR)、核磁共振碳谱(13CNMR)高分辨质谱(HRMS)分析确证.合成抗疟药伯氨喹的杂质A及其盐酸盐的路线方法是国内外首创,操作简单,原料廉价,易于实现工业化生产.In this paper,antimalarial drug primaquine related compound A and its hydrochloride was synthesized vio michael condensation,demethylation,acyl chlorination,amidation,carbonylation reduction,nitro reduction and aminohydro-chlorination in sequence from nitroethane and methyl acrylate as the starting compounds. The products were characterized by 1H NMR,13C NMR and HRMS. This route method was pioneered at home and abroad,simple in operation and cheap in raw material. This route method was also easy to realize the industrial production.

关 键 词：抗疟药 伯氨喹的杂质A 盐酸盐 合成 

分 类 号：O626[理学—有机化学]