Abstract
An efficient copper-catalyzed tandem approach for the synthesis of 2-imino[1,3]benzothiazines by the reaction of easily accessible 2-aminoaryl acrylates with isothiocyanates via in situ thioamidation and concomitant chemoselective intramolecular thia-Michael addition is described. Intramolecular cyclization was selectively triggered by the nitrogen 'b' of the thiourea intermediate P. (C) 2014 Elsevier Ltd. All rights reserved.