Abstract：
Here we report an efficient access to high-value N-polyfluoroalkyl anilines, primary polyfluoroalkylamines and N,N-bis(polyfluoroalkyl)amines, via N-polyfluoroalkylation of sulfonamides and phthalimide derivatives using sulfuryl fluoride (SO2 F2 ). The in situ formation of polyfluoroalkyl fluorosulfonates from commercially available fluorinated alcohols and economical sulfuryl fluoride is highly advantageous given that some polyfluoroalkyl halides are ozone-depleting substances (ODS) regulated by the Montreal protocol. This general method is applied to the polyfluoroalkylation of a variety of sulfonamides, N-sulfonyl carbamates and phthalimide with a wide tolerance of functional groups. The process thus provides viable access for industry to N-(polyfluoroalkyl)anilines as well as primary and secondary N-(polyfluoroalkyl)amines, which are very valuable but not easily accessible building blocks for life science applications.
摘要：
在这里，我们报告了对高价值N-多氟烷基苯胺的有效访问，伯多氟烷基胺和N，N-双(多氟烷基)胺,通过使用磺酰氟(SO2F2)的磺酰胺和邻苯二甲酰亚胺衍生物的N-多氟烷基化。考虑到一些多氟烷基卤化物是由蒙特利尔议定书规定的臭氧消耗物质(ODS),由市售的氟化醇和经济的硫酰氟原位形成多氟烷基氟磺酸盐是非常有利的。这种通用方法适用于各种磺酰胺的多氟烷基化，N-磺酰基氨基甲酸酯和邻苯二甲酰亚胺具有广泛的官能团耐受性。因此，该方法为工业提供了N-（多氟烷基）苯胺以及N-（多氟烷基）伯胺和仲胺的可行途径，这是非常有价值的，但不容易获得的构建块的生命科学应用。
