One-Pot Aminomethylation of Heteroarenes by Rongalite as <i>In Situ</i> C1 Source

Rongalite-mediated one-pot aminomethylation of heteroarenes using secondary amines/anilines has been developed. This transition-metal-free and mild reaction offers an efficient way to synthesize aminomethylated heteroaromatic compounds with high yields and broad functional group tolerance. Here, Rongalite plays a key role in generating the C1 unit source <i>in situ</i>, which triggers the aminomethylation process. This approach provides a library of aminomethylated imidazo[1,2-<i>a</i>]pyridines and imidazo[2,1-<i>b</i>]thiazoles.