Iridium(III)-Catalyzed Alkynylation of 2-(Hetero)arylquinazolin-4-one Scaffolds via C-H Bond Activation.

J Org Chem

CSIR-National Chemical Laboratory , Division of Organic Chemistry , Dr. Homi Bhabha Road , Pune 411008 , India.

Published: March 2019

The directed C-H alkynylation of 2-(hetero)arylquinazolin-4-ones has been explored with the ethynylbenziodoxolone reagent TIPS-EBX employing an Ir(III) catalyst. Complementary conditions for either monoalkynylation or dialkynylation have been developed. Also demonstrated is the broad scope of this reaction and the compatibility of various functional groups such as -F, -Cl, -Br, -CF, -OMe, -NO, and alkyl, etc.

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http://dx.doi.org/10.1021/acs.joc.8b02738DOI Listing

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