Indium-mediated 1,2-addition of iododifluoromethyl ketones with α, β-unsaturated ketones

A novel indium-mediated difluoroalkylation of iododifluoromethyl ketones with alpha, beta-unsaturated ketones, which provides an obviously significant route to access 1,2-addition product with excellent regioselectivity. This method has a wide range of substrate scope, good efficiency, and mild reaction conditions. In addition, this method was applied to the synthesis of difluoro derivatives of biologically active molecules containing unsaturated ketone structures, which might be served as potentially valuable fluorinated intermediates in drug discovery. (C) 2022 Elsevier Ltd. All rights reserved.

Automated summary

The novel indium-mediated difluoroalkylation of iododifluoromethyl ketones with alpha, beta-unsaturated ketones provides a significant route to access 1,2-addition product with excellent regioselectivity. This method has a wide substrate scope, high efficiency, and mild reaction conditions. Furthermore, it can be applied to the synthesis of difluoro derivatives of biologically active molecules containing unsaturated ketone structures, serving as potentially valuable fluorinated intermediates in drug discovery.