Two-step synthesis of aza- and diazaindoles from chloroamino-N-heterocycles using ethoxyvinylborolane

Abstract

(Chemical Equation Presented) 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. © 2009 American Chemical Society.