正丁基锂制备2-腈基-5-吡啶硼酸及其频那醇酯

Synthesis of 2-cyanopyridine-5-boronic Acid and Its Pinacol Ester By Improved n-butyllithium Protocol

以2-腈基-5-溴吡啶、三异丙基硼酸酯和正丁基锂为原料,用改良的Li-Br交换反应制备2-腈基-5-吡啶硼酸的方法,收率75%。其频那醇酯也方便地以2-腈基-5-吡啶硼酸和频那醇在甲苯中通过共沸脱水制备,收率81%。

Using 2 - cyano - 5 - bromopyridine, triisopropylboroate and n - butyllithium as material by an improved protocol where n - butyllithium is added to the mixture of 2 - cyano - 5 - bromopyridine and tri- isopropylboroate in toluene -THF（3 ： 1 ,v/v） ,the yield reach 75% after work - up. The 2 - cyanopyri- dine - 5 - boronie acid pinaco ester is prepared from 2 - cyanopyridine - 5 - boronic acid and pinacol in toluene by azeotropic dehydration the yield 81%.