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Practical Synthesis of Isocoumarins Via Rh(III)-catalyzed C-H Activation/annulation Cascade

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Specialty Chemistry
Date 2023 Feb 10
PMID 36761471
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Abstract

Herein, we report an unprecedented Rh(III)-catalyzed C-H activation/annulation cascade of readily available enaminones with iodonium ylides towards the convenient synthesis of isocoumarins. This coupling system proceeds in useful chemical yields (up to 93%) via a cascade C-H activation, Rh-carbenoid migratory insertion and acid-promoted intramolecular annulation. The success of gram-scale reaction and diverse functionalization of isocoumarins demonstrated the synthetic utility of this protocol.

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