Heterocycle Synthesis via Direct C–H/N–H Coupling

Abstract

A method for five- and six-membered heterocycle formation by palladium-catalyzed C–H/N–H coupling is presented. The method employs a picolinamide directing group, PhI­(OAc)₂ oxidant, and toluene solvent at 80–120 °C. Cyclization is effective for sp² as well as aliphatic and benzylic sp³ C–H bonds