An efficient synthesis of enantiomerically pure aromatic-fused N-containing heterocycles from common chiral aziridines

摘要

An efficient synthesis of enantiomerically pure aromatic-fused N-containing heterocycles was successfully achieved via Pd-catalyzed intramolecular C-N bond formation between the nitrogen originated from the aziridine and the halogen containing aromatic carbon. This reaction has a broad substrate scope to provide various enantiomerically pure (3,4-dihydro-2H-benzo[b][1,4]oxazin-3-yl) methanols, 2-hydroxymethyl-1,2,3,4-tetrahydroquinolines and (1,2,3,4- tetrahydroquinoxalin-2-yl)methanols from common chiral aziridines in good yields.