Dehydrogenative Cycloisomerization/Arylation Sequence of N‐Propargyl Carboxamides with Arenes by Iodine(III)‐Catalysis.

Dehydrogenative cycloisomerization/arylation sequence of heteroatom nucleophile‐tethered unactivated alkynes provides a facile and powerful approach to C−C bond formation between the generated heterocycles and unfunctionalized arenes. Here, we describe a hypervalent iodine(III)‐catalyzed synthesis of oxazoles concomitant with the introduction of aryl groups into side chain from N‐propargyl carboxamides and arenes, representing first C(sp3)−C(sp2) bond formation by the catalytic dehydrogenative cycloisomerization/arylation reaction in exo‐dig modes. [ABSTRACT FROM AUTHOR]