Sun Fei, Zheng Yiyi, Wu Mingxia, Ji Hongsen, Jiang Zhongyao, Liu Chenglin, Wu Xin-Xing
College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019, P. R. China.
Chem Commun (Camb). 2024 Jul 30;60(62):8075-8078. doi: 10.1039/d4cc02591a.
A mild Pd-catalyzed three-component cascade cyclization functionalization of -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 a borylation process to give versatile boryl-functionalized indene skeletons in a selective fashion. Significantly, (Bpin), (Bneop) and CH(Bpin) as boron sources are all tolerated. Additionally, the synthetic utility of this approach is demonstrated by gram-scale synthesis and synthetic transformations.
本文报道了一种温和的钯催化的三组分串联环化官能团化反应，该反应涉及碘代苯乙烯、内炔烃和硼试剂。该转化过程由分子间碳钯化、分子内Heck型环化和硼化过程的可控反应序列驱动，以选择性的方式生成通用的硼基官能化茚骨架。值得注意的是，作为硼源的(Bpin)、(Bneop)和CH(Bpin)均能耐受。此外，通过克级规模合成和合成转化证明了该方法的合成实用性。
