One-Pot Aminomethylation of Heteroarenes by Rongalite as In Situ C1 Source

Abstract

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 in situ, which triggers the aminomethylation process. This approach provides a library of aminomethylated imidazo[1,2-a]pyridines and imidazo[2,1-b]- thiazoles.