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目的 改进盐酸阿比朵尔的合成方法 .方法 以1,2-二甲基-5-羟基-3-吲哚甲酸乙酯为起始原料,经酰化、溴化、缩合、Mannich反应、成盐5步反应,得到目标产物盐酸阿比朵尔,目标产物及各步中间体结构经 LC-MS、1H-NMR确证.结果与结论 该合成工艺总收率为39.70% (以1,2-二甲基-5-羟基-3-吲哚甲酸乙酯计),较文献收率提高了 5. 1%,纯度大于99. 9% ,新工艺中不再使用一类溶剂四氯化碳和剧毒品苯硫酚,反应条件温和,适合工业化生产.“,”Influenza is an acute respiratory tract infection caused by influenza viruses and it remains a serious health concern. The antiviral activity of arbidol, a new antiviral agent, is most pronounced against influenza of the A and B antigenic type. In this paper, we optimized the synthetic process of arbidol hydrochloride(AH). There is a problem of using highly toxic solvents and raw materials in the reference method. On the basis of reference method, the reaction conditions such as reaction temperature and solvent were optimized. Arbidol hydrochloride was produced from 1,2-dimethy 1-5-hydroxy-3-indolecarboxylate through acylation, bromination, condensation, Mannich reaction and salt formation. The structures of the produced and associated intermediates were validated by LCMS and 1H-NMR during the synthesis. With our optimized synthetic process,the purity of our product is more than 99. 9% and the overall yield of AH is 39. 70%(calculated by the amount of ethyl 1,2-dimethyl-5-hydroxy-3-indolecarboxylate),which was 5. 1% higher than the reported yield in previous literatures. Additionally,toxic reagents such as carbon tetrachloride and thiophenol were not included in the optimized synthetic route. Therefore, we provided a milder synthetic strategy which is suitable for industrial production.