含氮杂环二氟甲基化反应的初步探索

Difluoromethylation of Nitrogen Heterocycles

鏻盐在有机化学中应用十分广泛,能够作为试剂或者催化剂实现各种反应。基于二氟甲基鏻盐的反应性质,本文探究了含氮杂环与二氟甲基鏻盐的二氟甲基化反应。经研究发现,二氟甲基鏻盐在碳酸铯作用下可释放二氟甲基亲核物种,对氮杂环进行亲核加成,从而实现了对含氮杂环的二氟甲基化。并将产率筛至60%。其最优条件为以:碳酸铯为引发剂、乙酸乙酯为溶剂、在室温条件下反应18小时,分离即可获得产物。

Bismuth salts are widely used in organic chemistry and can be used as reagents or catalysts to achieve various reactions.Based on the reaction properties of difluoromethyl sulfonium salts,the difluoromethylation reaction of nitrogen-containing heterocycles with difluoromethyl sulfonium salts was investigated.It has been found that difluoromethyl sulfonium salt can release difluoromethyl nucleophilic species under the action of cesium carbonate and nucleophilic addition of nitrogen heterocycles,thereby achieving difluoromethylation of nitrogen-containing heterocycles.