An efficient one-pot sequential intermolecular aza-Michael addition and Pd-catalyzed intramolecular Buchwald-Hartwig α-arylation of secondary amines have been investigated, for the synthesis of tetrahydroisoquinolines. This method is simple and furnished products in very good yield and also successfully applied for the synthesis of novel aza-spirotricylcic ethers. © 2012 Elsevier Ltd. All rights reserved.