A facile and efficient Cu(I)-catalyzed one-pot synthesis of 2H-1,4-benzoxazin-3-(4H)-one derivatives has been developed. The condensation between 2-(o-haloaryloxy)acyl chlorides and primary amines followed by Cu(I)-catalyzed intramolecular C-N bond coupling afforded a variety of 2H-1,4-benzoxazin-3-(4H)-ones in good to excellent yields. Diversified substitutents on the 4-position could be conveniently introduced.
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