Abstract
Traditional procedures toward 2-fluoromalonates tend to meet overfluorination. Herein, we describe a mild and efficient palladium-catalyzed carbonylative strategy for the synthesis of dialkyl 2-fluoromalonate derivatives avoided the mentioned challenges. By this new procedure, a range of malonates and difluoromalonate derivatives were prepared with good functional-group tolerance and excellent chemoselectivity. This procedure can also be applied in the late-stage carbonylation of various bioactive molecules. Furthermore, a low-pressure experiment and two scale-up reactions were performed smoothly in good to excellent yield.
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