Abstract

AbstractWe have developed an efficient and convenient strategy for the synthesis of pentasubstituted meta‐fluoropyridines. The annulation‐aromatization cascade reaction between trifluoromethyl ketimines and maleimides was promoted by N‐methyl‐2,2,6,6‐tetramethylpiperidine (PMP) in moderate to high yields. In this approach, two C−F bond cleavages happened in both [4+2] cycloaddition and aromatization separately. The pentasubstituted meta‐fluoropyridines could be reduced to tertiary amines by BH3 in moderate yield.

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