Synthesis of 5-halo-4h-1,3-oxazine-6-amines by a copper-mediated domino reaction

Abstract

Three become one! In one copper-mediated step, three simple components, including a propargylcarboxamide, a protected amine, and a source of chloride, assemble to give highly functionalized oxazines, which are interesting building blocks for the synthesis of other aminooxazine derivatives (see scheme; R 1=range of aryl or alkyl groups, R2=alkyl, EWG=electron-withdrawing group). © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.