Pd/C-catalyzed synthesis of N-aryl and N-alkyl isoquinolones via C-H/N-H activation

Pd/C-catalyzed direct synthesis of N-aryl and N-alkyl isoquinolones was developed via the annulationreactions of benzamides and alkynes in high yields (up to 99%) through the cleavage of C-H/N-H bonds. The reaction was ligand-free and air was used as oxidant. High regioselectivities were found when unsymmetrical alkynes or meta-benzamides were used as substrates. The heterocyclic carboxamide substrates, such as furan and thiophene derivatives, also afforded the corresponding products in high yields. (C) 2017 Elsevier B.V. All rights reserved.