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Annulative Coupling of Sulfoxonium Ylides with Aldehydes and Naphthols or Coumarins: Easy Access to Fused Dihydrofurans

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Figshare2025-01-17 更新2026-04-28 收录
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We present a novel, metal- and additive-free method for the robust synthesis of dihydrofuran-fused naphthalenes and coumarins. This approach utilizes the annulative coupling of sulfoxonium ylides with aldehydes, naphthols, or coumarins at ambient temperature. The method exhibits broad substrate compatibility, accommodating various functional groups on sulfoxonium ylides and naphthol or coumarin derivatives and resulting in good to high yields of the desired products. Additionally, we successfully scaled up the reactions, and the synthesized derivatives were further converted to other valuable bioactive molecules, validating the viability of our approach.

本研究报道了一种新颖的无金属、无添加剂方法,用于稳健合成二氢呋喃稠合萘(dihydrofuran-fused naphthalenes)与香豆素(coumarins)。该策略利用锍叶立德(sulfoxonium ylides)与醛、萘酚或香豆素在室温条件下发生环化偶联反应。此方法展现出宽泛的底物兼容性,可兼容锍叶立德、萘酚或香豆素衍生物上的多种官能团,目标产物收率可达良好至较高水平。此外,本研究成功实现了该反应的放大制备,且所合成的衍生物可进一步转化为其他具有高价值的生物活性分子,验证了该方法的实用性。

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2025-01-17
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