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◆ Organic Letters2026-05-07· Chemistry

Electrochemically Driven, p <i>K</i> <sub>a</sub> -Controlled Regioselective Selenocyclization: Synthesis of Isocoumarin-1-imines with Structural Validation

R N Zhang, Yi Zhou, Zhanzhou Wei, Yunfei Zhang

原始摘要(英文原文)· Original abstract
This study presents an electrochemical strategy that leverages the p K a of N -substituents to achieve precise regiocontrol in the selenocyclization of 2-alkynylbenzamides, providing efficient access to 4-selenyl isocoumarin-1-imines. This method successfully overcomes the longstanding selectivity challenges between competitive O / N -attack cyclization pathways. Crucially, the structure of the O -cyclized product was unambiguously confirmed by X-ray crystallographic analysis. Density functional theory (DFT) calculations further rationalize the observed high regioselectivity, revealing a significantly lower energy barrier for the O -attack pathway. The gram-scale synthesis and preliminary bioassays for fungicidal activity demonstrate the potential applications of this method.
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Electrochemically Driven, p <i>K</i> <sub>a</sub> -Controlled Regioselective Selenocyclization: Synthesis of Isocoumarin-1-imines with Structural Validation — 科研速览 Science Skim