A Palladium-Catalyzed Synthesis of Amidines from Aryl Halides

Abstract

Tin-free three-component coupling: Palladium-catalyzed coupling between aryl or heteroaryl bromides, primary or secondary amines, and tert-butyl isocyanide gives high yields of pharmaceutically interesting arylamidines [Eq. (1)]. dppf=1,1′-bis(diphenylphosphanyl)ferrocene; R1/R2=Bu/H, Ph/H, −(CH2)4−.