C-substituted morpholines and morpholinones are important building blocks in organic synthesis and pharmacophores in medicinal chemistry, however, diverse C3-disubstituted morpholines/morpholinones remain difficult to access. Here, the authors develop a facile construction of C3-disubstituted morpholinone bearing an aza-quaternary center achieved by ZnCl2-catalyzed cyclizative 1,2-rearrangement.
- Xing-Zi Li
- Yu-Ping He
- Hua Wu
