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H2SO4 catalyzed tandem alkylation-hydrolysis reaction of β-ethylthio-β-indolyl-α, β-unsaturated ketones and alcohols has been developed to access α-alkylated 3-aroylacetylindoles in up to 90% yield. Subsequent debenzoylation of α-alkylated 3-aroylacetylindoles in the presence of 1.0 equivalent of NaOH provides 3-arylpropionylindoles in excellent yields. The facile accessibility of various valuable α-alkylated 3-aroylacetylindoles and 3-arylpropionylindoles demonstrates the high practicability of this method.
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Zhang et al. (2026) studied this question.
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