Synthesis of N‐Aryl‐2‐substituted Tetrahydrobenzimidazoles via Direct N‐Arylation

Abstract

A series of novel N-aryl-2-substituted tetrahydrobenzimidazoles has been synthesized via direct N-arylation of 2-substituted tetrahydrobenzimidazoles, which was accomplished by a medium aryl electrophile, 4-methylsulfonylfluorobenze, in the presence of 37% KF/Al 2 O 3 and 18-crown-6 in fair yields under mild reaction conditions. Meanwhile, the hydrogenation of 2-phenylbenzimidazole was studied.