A variety of substituted enamine derivatives were first found to be conveniently converted to the corresponding 2H-azirines mediated by phenyliodine (III) diacetate (PIDA). The formed 2-aryl-2H-azirines could be applied in the synthesis of indole-3-carbonitriles or isoxazoles via thermal rearrangements.
Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China.