Regioselective oxidative C–H heptafluoroisopropylation of heteroarenes with heptafluoroisopropyl silver

Abstract

While CF(CF₃)₂-containing arenes are prevalent in pharmaceuticals and agrichemicals, CF(CF₃)₂-containing heteroarenes remain largely underexplored. Herein, we disclose the first oxidative C–H heptafluoroisopropylation of heteroarenes using AgCF(CF₃)₂ as the CF(CF₃)₂ source and ceric ammonium nitrate (CAN) as the oxidant. This protocol provides a practical and efficient approach towards a diverse array of CF(CF₃)₂-substituted heteroarenes with excellent regioselectivity. The synthetic utility of this protocol is well documented in the late-stage heptafluoroisopropylation of pharmaceutical molecules.