This method demonstrates palladium-catalyzed heteroannulation of alkynes, yielding regioselective C2-borylated indoles.
We report the synthesis of 2-indolylboramides via a palladium (Pd)-catalyzed heteroannulation of 2-iodoaniline derivatives and Bdan-capped alkynes (Bdan, 1,8-diaminonaphthalene boronamide). The process is highly regioselective, affording a diverse range of C2-borylated indoles. The synthetic utility of the process is demonstrated through the concise synthesis of the Tetradium alkaloid skeleton.
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Roberts et al. (2025) studied this question.
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