Domino aziridine ring opening and Buchwald-Hartwig type coupling-cyclization by palladium catalyst

Highly important trans-3,4-dihydro-2H-1,4-benzoxazine moieties were easily synthesized by domino aziridine ring opening with o-bromophenols and o-chlorophenols followed by the palladium catalyzed coupling-cyclization (intramolecular C (aryl)-N (amide) bond formation) with good to excellent yields. © 2012 Elsevier Ltd. All rights reserved.