Synthesis of 3-substituted-4 H-1,4-benzoxazines

Various 3-substituted-4 H-1,4-benzoxazines were prepared in good yields by lithiation-electrophilic substitution of the 4-Boc-4 H-1,4-benzoxazine. The synthesis of this carbamic derivative, in four steps from 2-aminophenol, was described.