A novel strategy has been introduced for the selective activation of the N–C(O) moiety in primary aromatic amides through the utilization of pyrylium tetrafluoroborate under mechanochemical conditions, where the amide group undergoes subsequent activation and is selectively substituted with the CF₃ or OCF₃ functionality. The scope of the present protocol includes selective transformation of diversely substituted aromatic amides into the respective trifluoromethyl and trifluoromethoxy arenes via mechanochemically induced deaminative functionalization under the synergy of a piezoelectric material barium titanate (BaTiO₃) and ruthenium-catalysis. The presented mechanochemical approach unlocks new chemical spaces in the pharmaceutical industry with an emphasis on PASE (pot, atom, and step economy) synthesis.

中文翻译：

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钌催化下酰胺基团向 OCF3 和 CF3 官能团的机械化学脱羰基转变


通过在机械化学条件下利用四氟硼酸吡啶，引入了一种选择性活化伯芳香酰胺中 N-C（O） 部分的新策略，其中酰胺基团经过后续活化并选择性地被 CF3 或 OCF3 官能团取代。本方案的范围包括在压电材料钛酸钡 （BaTiO3） 和钌催化的协同作用下，通过机械化学诱导的脱酰胺官能化将多种取代的芳香酰胺选择性转化为各自的三氟甲基和三氟甲氧基芳烃。所提出的机械化学方法以 PASE（罐、原子和步骤经济）合成的观点为制药行业开辟了新的化学空间。