One-Step Synthesis of α-Chloroaceto-phenones from Aryl Precursors

Significance

The authors reported herein a simple synthetic method for the preparation of α-chloro- and α-alkoxyacetophenones via the metallation of an aryl ring or a halogen-lithium exchange reaction, followed by the copper-catalyzed acylation of the corresponding arylzinc species. This reaction is suitable for the preparation of α-chloroacetophenones, which is otherwise difficult to achieve, as well as various alkoxyacetylaceto­phenones. Those are useful synthetic intermediates. This method therefore is complementary to the conventional Friedel-Crafts acylation.