A Metal-Free C-H Amination-Based Strategy for N-Amino Indole Synthesis

Matteo Corrieri,Lucia De Crescentini,Fabio Mantellini,Giacomo Mari,Stefania Santeusanio,Gianfranco Favi

EUROPEAN JOURNAL OF ORGANIC CHEMISTRY（2023）

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摘要

An oxidative cyclization of electron-rich alpha-arylhydrazones promoted by phenyliodine bis(trifluoroacetate) (PIFA) has been accomplished. This metal-free, chemoselective transformation allows to obtain synthetically and medicinally important N-amino-1H-indoles, obviating the need for pre-functionalization of substrates.

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关键词

cyclization,C(sp2)−H amination,indoles,hydrazones,hypervalent iodine(III) reagent

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