3-羧基-5-氟苯基硼酸的合成工艺研究

Research Progress on Synthesis of 3-borono-5-fluorobenzoic Acid

3-羧基-5-氟苯基硼酸是一种重要的有机合成中间体,可通过suzuki芳基偶联反应合成多烯烃、苯乙烯和联苯的衍生物,从而应用于众多天然产物、有机材料的合成中。本文以5-氟-3-溴甲苯为原料,利用两步反应合成目标产物的合成工艺:1利用有机锂试剂法合成3-氟-5-甲基苯硼酸;2将3-氟-5-甲基苯硼酸经过氧化反应合成目标产物,总产率为75.5%。本合成路线操作简单,原料的价格低,符合工业化生产的要求,可以进行工业化生产。

3- borono- 5- fluorobenzoic acid is an important intermediate for organic synthesis,widely used in organic synthesis,by suzuki aryl- coupling reaction synthesis of olefins,styrene and biphenyl derivative,which is applied to the synthesis of many natural products,organic materials. The use of a two- step reaction synthesis of the target product synthesis process was described using organic lithium reagent synthesis of（ 3- fluoro- 5- methylphenyl） boronic acid. The target product was synthesized using（ 3- fluoro- 5- methylphenyl） boronic acid through the oxidation reaction,the total yield was 75. 5%. This synthetic route is simple with low price of raw material,and accord with the requirement of industrial production to industrial production.