2-二氟甲氧(硫)基吡啶-5-硼酸频哪醇酯类化合物的合成  

Synthesis of 2-difluoromethoxy(thio)pyridine-5-boronic acid pinacol esters

作　　者：吴清梅 张秋艳 黄朋越 周志旭[1,2] WU Qing-mei;ZHANG Qiu-yan;HUANG Peng-yue;ZHOU Zhi-xu(School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China;School of Chemistry and Chemical Engineering,Guizhou University,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州省合成药物工程实验室,贵州贵阳550025 [3]贵州大学化学与化工学院,贵州贵阳550025

出　　处：《化学研究与应用》2021年第4期731-734,共4页Chemical Research and Application

基　　金：贵州省科技计划项目(黔科合基础[2020]1Y393)资助。

摘　　要：以吡啶类化合物作为起始原料,先经二氟甲基化反应在羟基或巯基上引入二氟甲基基团,再用铱催化剂活化吡啶环的C-H并直接引入硼酸频哪醇酯基团,得到目标化合物,其产物结构经^(1)H NMR、^(13)C NMR、MS和元素分析确证。该方法具有合成路线较短、反应条件温和、原料廉价易得以及产率较高等优点。Using pyridine compounds as starting materials,first difluoromethyl groups on hydroxyl or mercapto groups was introduced through difluoromethylation reaction,then iridium catalyst was used to activate pyridine ring CH and boronic acid pinacol ester groups was directly introduced to obtain the target compounds,which were confirmed by ^(1)H NMR,^(13)C NMR,MS and elemental analysis.The method had the advantages of short synthetic route,mild reaction conditions,cheap and easily available raw materials,and high yield.

关 键 词：二氟甲基 硼酸酯化合物 铱催化剂 合成 

分 类 号：O626[理学—有机化学]