Dihydrobenzisoxazoles are readily prepared in good yields by the [3+ 2] cycloaddition of oxaziridines and arynes. The reaction involves an unusual cleavage of the C− O bond of the oxaziridine and tolerates a variety of substituents on the oxaziridine and the o-(trimethylsilyl) aryl triflate to form aryl-, heteroaryl-, alkyl-, and naphthyl-substituted dihydrobenzisoxazoles. The resulting halogen-substituted dihydrobenzisoxazoles are readily elaborated to more ...
