Abstract

An acid-promoted multicomponent reaction for the direct C(sp3)N bond formation was achieved through intermolecular allylic amidation in a one-pot operation to synthesize 7-acetamido tetrahydroindole derivatives from simple and readily available arylglyoxal monohydrates, acetonitriles, and enamines of 5,5-dimethyl-1,3-cyclohexadione (dimedone) has been developed. Here acetonitrile acts both as solvent and reagent. These tetahydroindole derivatives are formed through domino condensation of the enamines and arylglyoxals followed by annulation and allylic amidation.

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