依曲替酸关键中间体4-甲氧基-2,3,6-三甲基苯甲醛的合成  

Synthesis of 4-methoxy-2,3,6-trimethylbe nzaldehyde-the key intermediate of acitretin

作　　者：张爱贵 王玉良[1,2] 

机构地区：[1]四川大学生命科学学院,四川成都610064 [2]四川大学化学学院,四川成都610065

出　　处：《化学研究与应用》2016年第5期731-734,共4页Chemical Research and Application

摘　　要：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.

关 键 词：依曲替酸 Hagemann酯 芳香异构化 4-甲氧基-2 3 6-三甲基苯甲醛 

分 类 号：O625.4[理学—有机化学]