A Convenient Procedure for the Formylation of Amines and Alcohols Using Cyanomethyl Formate

Abstract

Abstract A simple method for the direct formylation of amines using cyanomethyl formate is described. The formylation succeeds in moderate to high yields under mild and neutral conditions. Thus, formamides 2a-f, 2i-m are obtained at room temperature. A chemoselective N-formylation is achieved in the case of ethanolamine. The formylation of nitroanilines and the O-formylation of alcohols only succeeds in the presence of a catalytic amount of imidazole leading to 2g,h and 3a-e, respectively.