A hypervalent iodine(III)-mediated C(sp)-C(sp) bond functionalization reaction for the formation of C-C, C-P, and C-H bonds in dihydroquinazolines has been developed. This one-pot method involves successive oxidation of dihydroquinazoline substrates, mesolytic cleavage of a -butyl substituent, and bond formation to a variety of nucleophiles in moderate to high yields.
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