Hexafluoroisopropanol/trifluoromethanesulfonic acid assists the synthesis of 3-(2-chloropyrimidin-4-yl)-1H-indoles

Abstract

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.