Selective alkylation of 2-pyridone could solve a challenge in chemistry and streamline the synthesis of important molecules. Here we report the regioselective O-alkylation of 2-pyridones by TfOH-catalyzed carbenoid insertion. In… Click to show full abstract
Selective alkylation of 2-pyridone could solve a challenge in chemistry and streamline the synthesis of important molecules. Here we report the regioselective O-alkylation of 2-pyridones by TfOH-catalyzed carbenoid insertion. In the catalytic system, alkylation of 2-pyridone was achieved with unprecedented regioselectiviy (>99 : 1). This protocol is characterized by mild reaction conditions, metal-free, and simplicity. Moreover, this method provides the desired products in good yield and demonstrates a broad substrate scope in this transformation.
               
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