Palladium-catalyzed synthesis achieves high regioselectivity in N-heterocycles, suggesting a robust method for diverse scaffold construction.
As privileged structural motifs, the efficient synthesis of multifused N-heterocycles remains highly challenging. Here, we report a palladium-catalyzed intramolecular hydroarylation of N-alkynyl indoles bearing an electron-withdrawing group at the 2-position. This reaction proceeds in high yield (up to 95%) and excellent regioselectivity, producing six-membered, indole-annulated sulfur/phosphorus heterocycles. This method offers a robust and efficient protocol for constructing these valuable scaffolds.
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Li et al. (2025) studied this question.
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