Rh(iii)-Catalyzed acylation of heteroarenes with cyclobutenones via C-H/C-C bond activation.

Rhodium(iii)-catalyzed C-H acylation of heteroarenes has been realized using cyclobutenones as an acylating reagent. This coupling proceeded via integration of C-H activation of heteroarenes and C-C cleavage of cyclobutenones. The reaction features excellent regio/chemoselectivity leading to versatile chalcones with exclusive E-selectivity.