The C-H activation/1,3-diyne strategy: Highly selective direct synthesis of diverse bisheterocycles by RhIII catalysis

Abstract

The reactivity and selectivity of 1,3-diynes in transition-metal-catalyzed C-H activation is exploited to quickly assemble diverse polysubstituted bisheterocycles, which are highly important but difficult to access. By using the C-H activation/1,3-diyne strategy, we overcame the challenges of selectivity (chemo-, regio-, and mono-/diannulation) and constructed seven kinds of adjacent bisheterocycles through the formation of four strategic bonds with high efficiency and high selectivity. Di-verse: The use of the C-H activation/1,3-diyne general strategy allowed the challenges of selectivity (chemo-, regio-, and mono-/diannulation) to be overcome. This allowed direct construction of diverse polysubstituted bisheterocycles, which are highly important but difficult to access, through the formation of four strategic bonds with high efficiency and high selectivity. © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.