设计了一种新的合成依曲替酸关键中间体4-甲氧基-2,3,6-三甲基苯甲醛的方法.以Hagemann酯为原料,通过碳3位上的甲基化,芳香异构化,还原以及氧化共4步反应合成了目标化合物.所得到的化合物经过核磁共振氢谱,碳谱以及质谱确认,总收率达到49%.本合成路线原料廉价易得,操作简便,反应条件相对温和.%A new method for the synthesis of the 4-methoxy-2,3,6-trimethylbenzaldehyde,a key intermediate of acitretin,was a-chieved from Hagemann' s ester in four steps including methylation at C-3 position,aromatic isomerization,reduction and oxidation. The obtained compounds were characterized through 1 H NMR,13 C NMR and MS. The overall yield of the synthetic route was 49%. The raw materials used in this synthetic route were cheap and readily available while the reaction conditions were relatively mild.
展开▼