【摘要】 目的 探讨合成茚地普隆的方法。方法 以2-乙酰噻吩为原料，经过DMFDMA缩合反应，羟胺盐酸盐及氨基胍硝酸盐参与的环合反应及N-甲基化反应，乙酸条件回流的环合等共七步反应，合成了目标化合物Indiplon，并对原工艺进行了改进。结果及结论 目标化合物的总收率为40.6%，结构经质谱、核磁共振氢谱及元素分析等确正，本路线反应条件温和，原料来源方便，成本低，适合工业化生产。

    【关键词】 药物化学;制备;化学合成

    An improved synthesis method of indilplon

    SHAO Qiu-rong,WU Jin-chang.Shunde Entry-Exit Inspection and Quarantine Bureau Agricultural and Chemical Products Laboratory,Shunde 528303,China

    【Abstract】 Objective To synthesis indiplon.Methods The synthesis started from commercially available of 2-acetylthiophene and dimethylformamide dimethyl acetal by a sequence of reactions including condensation,cyclization, N-methylation.Rusults and Conclusion The overall yield of the synthesis is 40.6%.This approach is industrially applicable for the production of indiplon characterized by its commercially available starting materials, easy purification processes for the synthetic intermediates and highly overall yield of the final product. ......