A mild Pd-catalyzed three-component cascade cyclizaiton functionalization of o-iodostyrenes, internal alkynes and boron reagents is presented. The transformation is driven by a controlled reaction sequence of intermolecular carbopalladation, intramolecular Heck-type cyclization, and borylation process to give the versatile boryl-functionalized indene skeletons in a selective fashion. Significantly, (Bpin)2, (Bneop)2 and CH2(Bpin)2 as boron sources are all tolerated. Additionally, the synthetic utility of this approach is demonstrated by gram-scale synthesis and synthetic transformations.

中文翻译：

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三组分级联碳钯化/Heck环化/硼化：轻松获得硼基官能化茚


提出了邻碘苯乙烯、内炔烃和硼试剂的温和 Pd 催化三组分级联环化官能化。该转化是由分子间碳钯化、分子内 Heck 型环化和硼基化过程的受控反应序列驱动的，以选择性方式产生多功能的硼基官能化茚骨架。值得注意的是，(Bpin)2、(Bneop)2 和 CH2(Bpin)2 作为硼源都是可以容忍的。此外，这种方法的合成效用通过克级合成和合成转化得到了证明。