The functionalization of cyclic ethers has received significant attention; however, the skeletal editing of cyclic ethers via O-to-N exchange remains challenging. Herein, we report a R3P/ICH2CH2I-promoted O-to-N exchange of cyclic ethers. This strategy enables the direct conversion of widely available cyclic ethers─such as tetrahydrofuran and 1,4-dioxane─into nitrogen-containing heterocycles, structural motifs commonly found in biologically active molecules. The method exhibits broad compatibility with secondary and tertiary amines, delivering the corresponding products in moderate to good yields.
Zhang et al. (Sun,) studied this question.