To date, the general and catalytic α-arylation of cyclic 1,3-dicarbonyls remains elusive. We now report the first Rh-catalyzed α-arylation of cyclic 1,3-dicarbonyls with benzocyclobutenols through a cyclic iodonium ylide strategy. Our strategy represents a good solution for the previously challenging α-arylation of cyclic 1,3-dicarbonyls with sterically demanding aryl partners, which is especially appropriate for structurally unique heteroaromatic 1,3-dicarbonyls. Our approach features mild conditions, readily available starting materials, high yields, excellent functional group-tolerance, and simple operation, providing expedient access toward medically important 2-aryl (hetero)cyclic 1,3-dicarbonyls. The practicality of this approach is demonstrated by the gram-scale synthesis, one-pot synthesis, and numerous downstream transformations.

中文翻译：

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通过环状碘鎓叶立德策略实现环状 1,3-二羰基与苯并环丁烯醇的 Rh 催化 α-芳基化

迄今为止，环状 1,3-二羰基的一般催化 α-芳基化仍然难以捉摸。我们现在报道了第一个通过环状碘鎓叶立德策略，Rh 催化的环状 1,3-二羰基与苯并环丁烯醇的 α-芳基化反应。我们的策略为先前具有空间要求的芳基伙伴的环状1,3-二羰基的α-芳基化提供了一个很好的解决方案，这特别适合结构独特的杂芳族1,3-二羰基。我们的方法具有条件温和、起始原料易得、收率高、官能团耐受性优异且操作简单的特点，为获得医学上重要的2-芳基（杂）环1,3-二羰基提供了便利。克级合成、一锅合成和大量下游转化证明了该方法的实用性。