Synthesis of N-aryl derived formamides using triflic anhydride

Abstract

A facile and convenient one-pot protocol for the N-formylation of aryl amines has been furnished using Tf₂O. This approach involves N-formylation of anilines and its derivatives employing formic acid as a formyl source and triflic anhydride (Tf₂O) as an activator as the key step. This work highlights the ability of Tf₂O as an activating agent, includes operational simplicity, easy applicability to gram-scale preparation and to afford the N-formyl aryl amines in moderate to good yields.