This work mainly reports a method of selectively functionalizing indole compounds using hexafluoroisopropanol (HFIP)/CF₃SO₃H to promote electrophilic substitution of Lewis acid activated indoles, providing a new approach for the synthesis of 3-(2-chloropyrimidin-4-yl)-1H-indoles. Compared with the existing approaches, our work expands the capabilities of synthesizing different 3-(2-chloropyrimidin-4-yl)-1H-indoles, with high yields, and offers another practical approach for further development of important pharmaceutical intermediates. Moreover, more friendly conditions to the environment and better functional group tolerance showcase the practicality of this chemistry.

该工作主要报道了一种利用六氟异丙醇(HFIP)/CF ₃ SO ₃ H对吲哚类化合物进行选择性官能化以促进Lewis酸活化吲哚的亲电取代的方法，为3-(2-氯嘧啶-4-基)的合成提供了新的途径。 )-1 H-吲哚。与现有方法相比，我们的工作扩展了合成不同3-(2-氯嘧啶-4-基)-1 H-吲哚的能力，且收率高，为进一步开发重要的药物中间体提供了另一种实用方法。此外，对环境更友好的条件和更好的官能团耐受性展示了这种化学的实用性。