Key Laboratory of Biocatalysis & Chiral Drug Synthesis of Guizhou Province, Generic Drug Research Center of Guizhou Province, School of Pharmacy, Zunyi Medical University, Zunyi, Guizhou 563003, P. R. China.
Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, School of Pharmaceutical Sciences, Chongqing University, Chongqing 401331, P. R. China.
Org Lett. 2020 Apr 3;22(7):2816-2821. doi: 10.1021/acs.orglett.0c00809. Epub 2020 Mar 18.
To date, the iron-catalyzed construction of C-heteroatom bonds has been less developed due to the difficulty of transmetalation with heteroatom anions and the sluggish reductive elimination. Herein we report an iron-catalyzed method for the silylation of (hetero)aromatic chlorides. It features high efficiency, a broad substrate scope, and excellent functional group compatibility. Moreover, this protocol enables the late-stage silylation of some pharmaceuticals, thus providing an excellent method to access valuable intermediates in medicinal chemistry.
迄今为止,由于与杂原子阴离子的转金属化和缓慢的还原消除,铁催化的 C-杂原子键的构建发展较少。在此,我们报道了一种铁催化的(杂)芳基氯化物的硅化方法。它具有高效、广泛的底物范围和优异的官能团兼容性。此外,该方案还可以对一些药物进行后期硅化,从而为药物化学中获得有价值的中间体提供了一种极好的方法。