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. 2014 Sep 1;53(36):9650-4.
doi: 10.1002/anie.201403782. Epub 2014 Jul 1.

The C-H activation/1,3-diyne strategy: highly selective direct synthesis of diverse bisheterocycles by Rh(III) catalysis

Da-Gang Yu  1 , Francisco de Azambuja, Tobias Gensch, Constantin G Daniliuc, Frank Glorius
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The C-H activation/1,3-diyne strategy: highly selective direct synthesis of diverse bisheterocycles by Rh(III) catalysis

Da-Gang Yu et al. Angew Chem Int Ed Engl. .

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.

Keywords: CH activation; RhIII catalysis; alkynes; heterocycles; selectivity.

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