化学
亲核芳香族取代
三氟甲基
芳基
有机化学
戒指(化学)
亲电芳香族取代
四氟硼酸盐
组合化学
范围(计算机科学)
功能群
离子液体
亲核取代
催化作用
烷基
计算机科学
程序设计语言
聚合物
作者
Michał Jakubczyk,Satenik Mkrtchyan,Mohanad Shkoor,Suneel Lanka,Šimon Budzák,Miroslav Iliaš,Marek Skoršepa,Viktor O. Iaroshenko
摘要
Increased interest in the trifluoromethoxy group in organic synthesis and medicinal chemistry has induced a demand for new, selective, general, and faster methods applicable to natural products and highly functionalized compounds at a later stage of hit-to-lead campaigns. Applying pyrylium tetrafluoroborate, we have developed a mechanochemical protocol to selectively substitute the aromatic amino group with the OCF3 functionality. The scope of our method includes 31 examples of ring-substituted anilines, including amides and sulfonamides. Expected SNAr products were obtained in excellent yields. The presented concise method opens a pathway to new chemical spaces for the pharmaceutical industry.
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