Two-Step Synthesis of Aza- and Diazaindoles from Chloroamino-<i>N</i>-heterocycles Using Ethoxyvinylborolane

Abstract

An efficient two-step route to a broad range of aza- and diazaindoles was established, starting from chloroamino-N-heterocycles, without the need for protecting groups. The method involves an optimized Suzuki-Miyaura coupling with (2-ethoxyvinyl)borolane followed by acetic acid-catalyzed cyclization.