A convenient approach towards 2- and 3-aminobenzo[b]thiophenes

Reaction of 1-(2-chloro-5-nitrophenyl)ethanone via Willgerodt–Kindler route with primary or secondary amines and sulfur allows a simple, efficient one-pot synthesis of 3-aminobenzo[b]thiophenes. Base-catalyzed transformation of 4-(2-chloro-5-nitrophenyl)-1,2,3-thiadiazole in the presence of primary and secondary amines offers a convenient approach towards 2-aminobenzo[b]thiophenes.

Figure optionsDownload as PowerPoint slide