合成3-羟基-2-(4-吡啶基)-1H-茚-1-酮的工艺改进

Process Improvement on the Synthesis of 3-Hydroxy-2-(pyridin-4-yl)-1H-inden-1-one

以邻苯二甲酸酐和4-甲基吡啶为起始原料,正十二烷为溶剂,氯化锌为催化剂,于190℃反应24 h合成了抗癌药物瓦他拉尼的关键中间体——3-羟基-2-(4-吡啶基)-1H-茚-1-酮,收率90.6%,其结构经1H NMR,IR和MS确证。

An important intermediate of anti-cancer drug （ Vatalanib）, 3-hydroxy-2-（pyridin-4-yl） - 1H-inden-l-one, was synthesized by the reaction of phthalic anhydride with 4-picoline using choose dodecane as the solvent and ZnC12 as the catalyst at 190℃ for 24 h. The structure was confirmed by H NMR, IR and MS. The yield was 90.6%.