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A straightforward approach to the synthesis of 3-bromoindoles via palladium-catalyzed oxidative C-H activation/annulation of N-alkylanilines with bromoalkynes has been described. This protocol features high atom economy, excellent chemo- and regioselectivities, and good functional group tolerance. Moreover, the resultant 3-bromoindoles can be transformed to various functionalized indole derivatives, which demonstrates the practicability of this method in organic synthesis.
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Fang et al. (2022) studied this question.
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