3-乙酰氨基邻苯二甲酸酐的合成  

Synthesis of N-(1,3-dioxo-1,3-dihydrobenzofuran-4-yl)acetamide

作　　者：谢月红 周季颖 汪锦娟 XIE Yue-hong;ZHOU Ji-ying;WANG Jin-juan(Department of Pharmacy,Nanjing First Hospital,Nanjing Medical University,Nanjing 210000,China)

机构地区：[1]南京医科大学附属南京医院(南京市第一医院)药学部,江苏南京210000

出　　处：《精细化工中间体》2024年第6期29-31,共3页Fine Chemical Intermediates

摘　　要：3-乙酰氨基邻苯二甲酸酐是合成阿普斯特的关键中间体,以3-硝基邻苯二甲酸为起始原料,经环合、硝基还原、乙酰化制得,并对合成工艺进行了优化。优化条件下目标化合物总收率79.9%(以3-硝基邻苯二甲酸计),纯度98.9%(HPLC),目标化合物结构经ESI-MS、^(1)H NMR表征确证。制备方法操作简便,反应条件温和,所用起始物料及相关试剂便宜易得,可用于工业化生产。N-(1,3-dioxo-1,3-dihydrobenzofuran-4-yl)acetamide,the key intermediate of Apremilast was prepared from 3-nitrophthalic acid via cyclization,reduction,and acetylation.The reaction conditions were optimized for the synthesis of N-(1,3-dioxo-1,3-dihydrobenzofuran-4-yl)acetamide.The total yield of the target compound was improved to 79.9%with the purity of 98.9%(HPLC),and the structure of target compound was identified by ESI-MS and^(1)H NMR.The improved process is facile and suitable for industrial production with relatively convenient operation procedures,and easily available raw material.

关 键 词：阿普斯特 3-硝基邻苯二甲酸 合成 

分 类 号：R914[医药卫生—药物化学] TQ463[医药卫生—药学]