(4-(N-环丙基氨磺酰)-2,5-二氟苯基)硼酸的合成

Synthesis of (4-(N-cyclopropylsulfamoyl)-2,5-difluorophenyl)boronic Acid

(4-(N-环丙基氨磺酰)-2,5-二氟苯基)硼酸是一个重要的化工中间体,目前无合成路线报道。通过查阅文献制定了最佳合成路线,本文设计了一条以2,5-二氟溴苯为起始原料,经磺酰化、酰胺化和取代反应得到目标化合物的合成路线。通过大量平行实验,对温度、投料比例等实验因素进行考察,得出了最佳反应条件。该方法原料廉价易得,方法简单,操作简便,收率较高,适合工业化生产。

（4-（N-cyclopropylsulfamoyl）-2,5-difluorophenyl） boronic acid is an important pharmaceutical chemical intermediates, there is no synthesis route reported. The synthesis route of the target compound was obtained by the sulfonylation, amidation and substitution of 2,5-difluorobromobenzene as starting materials. Through a large number of parallel experiments, the temperature, feed ratio and other experimental factors were investigated, the best reaction conditions were obtained. The method has the advantages of low cost, simple method, simple operation and high yield, and is suitable for industrial production.