PDF(Pubmed)
Abstract：
Functionalized imidazo[1,2-α]pyridines are important scaffolds in pharmaceuticals. Herein, we present an efficient 3-sulfonylmethylation protocol for imidazo[1,2-α]pyridines by sodium sulfinates in DMA and H2O (2:1) via an FeCl3-catalyzed three-component coupling reaction. Various sulfonylmethyl imidazo[1,2-α]pyridines were thus afforded in high yields with excellent functional group tolerance. A plausible oxidation-addition mechanism was proposed.
摘要：
官能化咪唑并[1,2-α]吡啶是药物中重要的支架。在这里，我们通过FeCl3催化的三组分偶联反应，在DMA和H2O（2：1）中通过亚硫酸钠为咪唑并[1,2-α]吡啶提供了有效的3-磺酰基甲基化方案。因此，以高产率提供了各种磺酰基甲基咪唑并[1,2-α]吡啶，并具有出色的官能团耐受性。提出了一种合理的氧化加成机理。
