卡洛芬合成工艺研究

Synthesis of Carprofen

以环己烯酮和甲基丙二酸二乙酯为起始原料,经Fischer合成法与对氯苯肼盐酸盐环合,用氯酸钠氧化脱氢,水解得到兽用非甾体抗炎药卡洛芬,反应总收率为44.8%。该方法使用氯酸钠替代价格昂贵的DDQ、四氯苯醌等试剂氧化脱氢,使工艺更为简便、经济、绿色。

Carprofen was synthesized via cyclization of cyclohexenone,diethyl methylmalonate and 4-chlorophenylhydrazine,oxidative dehydrogenation by sodium clorate and hydrolysis.The overall yield of Carprofen is 44.8%.Sodium chlorate was used instead of expensive oxidizing reagent such as DDQ to make the process more convenient,economic,and green.