Abstract

Molecular iodine-promoted efficient construction of isatins from 2'-aminophenylacetylenes, 2'-aminostyrenes, and 2'-amino-β-ketoesters is developed via oxidative amidation of sp, sp(2), and sp(3) C-H bonds. The reaction involves consecutive iodination, Kornblum oxidation, and intramolecular amidation in a single reactor. The present method meets all of the atom and redox economy principles.

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