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Enantioselective Synthesis of Fused Isocoumarins via Palladium-Catalyzed Annulation of Alkyne-Tethered Malononitriles

Hui Zhang, Weishuang Li, Xudong Hu, Wen‐Bo Liu

2021The Journal of Organic Chemistry25 citationsDOI

Abstract

An enantioselective palladium-catalyzed annulation of alkyne-tethered malononitriles for the synthesis of 3,4-ring-fused isocoumarins is described. This cascade strategy involves oxypalladation of ortho-alkynylbenzoates and desymmetrizing addition onto one cyano group of the pendant malononitriles, which enables the concurrent construction of two rings and an all-carbon quaternary stereocenter in a single operation.

Topics & Concepts

IsocoumarinsAnnulationChemistryStereocenterEnantioselective synthesisAlkynePalladiumCatalysisRing (chemistry)Combinatorial chemistryStereochemistryOrganic chemistryCatalytic C–H Functionalization MethodsSynthesis and Biological ActivitySynthesis and Catalytic Reactions
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