Rhodium(III)-Catalyzed C–H Activation: Ligand-Controlled Regioselective Synthesis of 4-Methyl-Substituted Dihydroisoquinolones

Abstract

Rh-catalyzed C-H functionalization of <i>O</i>-pivaloyl benzhydroxamic acids with propene gas provides access to 4-methyl-substituted dihydroisoquinolones. Good to excellent levels of regioselectivity are achieved using [Cp^tRhCl₂]₂ as a precatalyst under optimized conditions. Thorough examination of aryl/heteroaryl <i>O</i>-pivaloyl hydroxamic acid substrates, ligand effects on C-H site selectivity, alkene scope, and demonstration of scale are discussed within.