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

Abstract 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( sp 3 )−C( sp 2 ) bond formation by the catalytic dehydrogenative cycloisomerization/arylation reaction in exo‐dig modes. magnified image