Abstract

Abstract A facile and direct synthetic method for the construction of alkoxyamine derivatives through copper-catalyzed aerobic oxidative activation of sp3 C–H bond was developed in good to excellent yields (75−95%), by treating the readily available 1,3-dicarbonyl compounds with 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and its derivatives. This method was also successfully applied to the preparation of quaternary α-fluorinated α-hydroxyl acid derivatives.

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